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Efavirenz pentyne analog
An impurity of Efavirenz. Efavirenz is an antiretroviral medication used for the treatment of HIV/AIDS. Synonyms: (S)-6-Chloro-4-(pent-1-ynyl)-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one. CAS No. 205755-86-8. Molecular formula: C14H11ClF3NO2. Mole weight: 317.69.
Efavirenz quinoline analog
An impurity of Efavirenz, a nonnucleoside HIV-1 reverse transcriptase inhibitor and antiviral agent. Synonyms: 2-Cyclopropyl-6-chloro-4-(trifluoromethyl)quinoline. Grade: > 95%. CAS No. 391860-73-4. Molecular formula: C13H9ClF3N. Mole weight: 271.67.
Efavirenz Related Compound B
An impurity of Efavirenz. Efavirenz is an antiretroviral medication used for the treatment of HIV/AIDS. Synonyms: Efavirenz ethene analog; (4S)-6-Chloro-4-[(1E)-2-cyclopropylethenyl]-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-Benzoxazin-2-one; USP Efavirenz Related Compound B. Grade: > 95%. CAS No. 440124-96-9. Molecular formula: C14H11ClF3NO2. Mole weight: 317.69.
EFdA-TP
EFdA-TP is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP inhibits HIV-1 RT with multiple mechanisms. Synonyms: 2'-Deoxy-4'-Ethynyl-2-Fluoroadenosine 5'-(Tetrahydrogen Triphosphate); Islatravir triphosphate. Grade: ≥98%. CAS No. 950913-56-1. Molecular formula: C12H15FN5O12P3. Mole weight: 533.19.
EFdA-TP tetraammonium
EFdA-TP tetraammonium is a potent inhibitor of nucleoside reverse transcriptase (RT). It inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetraammonium inhibits HIV-1 RT with multiple mechanisms. Grade: 95%. Molecular formula: C12H27FN9O12P3. Mole weight: 601.32.
EFdA-TP tetrasodium
EFdA-TP tetrasodium is a potent inhibitor of nucleoside reverse transcriptase (RT). EFdA-TP tetrasodium inhibits HIV-1 RT with multiple mechanisms. Molecular formula: C12H11FN5Na4O12P3. Mole weight: 621.12.
Efinaconazole
Efinaconazole is a triazole antifungal. It is approved for use in Canada and the USA as a 10% topical solution for the treatment of onychomycosis (fungal infection of the nail). Efinaconazole acts as a 14α-demethylase inhibitor. Efinaconazole inhibits fungal lanosterol 14α-demethylase involved in the biosynthesis of ergosterol, a constituent of fungal cell membranes. Efinaconazole has been shown to be active against isolates of the following microorganisms, both in vitro and in clinical infections. Efinaconazole exhibits in vitro minimum inhibitory concentrations (MICs) of 0.06 μg/mL or less against most ( ≥ 90%) isolates of the following microorganisms: Trichophyton rubrum; Trichophyton mentagrophytes. Synonyms: KP103; KP-103; KP 103; CTK5J2975; AGJ95634; KB145948; AGJ 95634; KB 145948; AGJ-95634; KB-145948; Efinaconazole; trade name: Jublia. Grade: >98%. CAS No. 164650-44-6. Molecular formula: C18H22F2N4O. Mole weight: 348.39.
Efinaconazole (2R,3R)-diol O-methanesulfonate
An impurity of Efinaconazole. Efinaconazole is a potent topical antifungal medication used primarily to treat onychomycosis (gray nail disease) caused by dermatophytes such as Trichophyton rubrum and Trichophyton mentagrophytes. Synonyms: 2,3-Butanediol, 2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-, 3-methanesulfonate, [R-(R*,R*)]-; (2R,3R)-3-(2,4-Difluorophenyl)-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butan-2-yl methanesulfonate; (2R,3R)-2-(2,4-Difluorophenyl)-3-methanesulfonyloxy-1-(1H-1,2,4-triazol-1-yl)-2-butanol; Efinaconazole Impurity 30. Grade: ≥95%. CAS No. 133775-26-5. Molecular formula: C13H15F2N3O4S. Mole weight: 347.34.
Efinaconazole 2R,3R Epoxy triazole
An enantiomer of Efinaconazole, a triazole antifungal approved to treat fungal infections of the toenails as a topical solution. Synonyms: 1-[[(2R,3R)-2-(2,4-Difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole; (2R-trans)-1-[[2-(2,4-Difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole. Grade: > 95%. CAS No. 135270-13-2. Molecular formula: C12H11F2N3O. Mole weight: 251.23.
Efinaconazole (2R,3R) Regiamer
An impurity of Efinaconazole, a triazole antifungal approved to treat fungal infections of the toenails as a topical solution. Synonyms: (2R,3R)-2-(2,4-Difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(4H-1,2,4-triazol-4-yl)butan-2-ol. Grade: 95%. CAS No. 2122222-10-8. Molecular formula: C18H22F2N4O. Mole weight: 348.4.
Efinaconazole (2R,3S) Distereomer
An impurity of Efinaconazole, a triazole antifungal approved to treat fungal infections of the toenails as a topical solution. Grade: 90%. CAS No. 2055038-60-1. Molecular formula: C18H22F2N4O. Mole weight: 348.4.
Efinaconazole (2S,3R) Distereomer
An impurity of Efinaconazole, a triazole antifungal approved to treat fungal infections of the toenails as a topical solution. Grade: 90%. CAS No. 2055038-61-2. Molecular formula: C18H22F2N4O. Mole weight: 348.4.
Efinaconazole 2S,3S Epoxy triazole
An enantiomer of Efinaconazole, a triazole antifungal approved to treat fungal infections of the toenails as a topical solution. Synonyms: 1-[[(2S,3S)-2-(2,4-Difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole; (2S-trans)-1-[[2-(2,4-Difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole. Grade: > 95%. CAS No. 135270-10-9. Molecular formula: C12H11F2N3O. Mole weight: 251.23.
Efinaconazole Diol triazole (2R,3R)
A useful synthetic intermediate in the synthesis of Efinaconazole. Synonyms: (2R,3R)-2-(2,4-Difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butane-2,3-diol Methanesulfonate. Grade: 90%. CAS No. 1175536-50-1. Molecular formula: C13H17F2N3O5S. Mole weight: 365.35.
Efinaconazole Diol triazole (2S,3R)
An impurity of efinaconazole. Efinaconazole is a triazole antifungal. Synonyms: (2S,3R)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butane-2,3-diol. Grade: 90%. CAS No. 135272-36-5. Molecular formula: C12H13F2N3O2. Mole weight: 269.25.
Efinaconazole-N-oxide
An impurity of Efinaconazole, a triazole antifungal approved to treat fungal infections of the toenails as a topical solution. Synonyms: 1-((2R,3R)-3-(2,4-Difluorophenyl)-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butan-2-yl)-4-methylenepiperidine 1-oxide. CAS No. 2055038-63-4. Molecular formula: C18H22F2N4O2. Mole weight: 364.4.
Efinaconazole Related Impurity 3
The S,S-enantiomer of Efinaconazole, a medication used to treat toenail infection caused by fungus. Synonyms: ent-Efinaconazole; (2S,3S)-Efinaconazole; (αS,βS)-α-(2,4-Difluorophenyl)-β-methyl-4-methylene-α-(1H-1,2,4-triazol-1-ylmethyl)-1-piperidine ethanol; [S-(R*,R*)]-α-(2,4-Difluorophenyl)-β-methyl-4-methylene-α-(1H-1,2,4-triazol-1-ylmethyl)-1-piperidine ethanol. Grade: > 95%. CAS No. 164650-45-7. Molecular formula: C18H22F2N4O. Mole weight: 348.39.
Efinaconazole Related Impurity 4
An enantiomer of Efinaconazole, a triazole antifungal approved to treat fungal infections of the toenails as a topical solution. Synonyms: Efinaconazole 2S,3R Epoxy triazole; 1-(((2S,3R)-2-(2,4-difluorophenyl)-3-methyloxiran-2-yl)methyl)-1H-1,2,4-triazole; 1-{[(2S,3R)-2-(2,4-difluorophenyl)-3-methyloxiran-2-yl]methyl}-1H-1,2,4-triazole; (2S,3R)-2-(2,4-difluorophenyl)-3-methyl-2-(1H-1,2,4-triazol-1-yl)methyloxirane. Grade: > 95%. CAS No. 135270-07-4. Molecular formula: C12H11F2N3O. Mole weight: 251.24.
Efinaconazole THP DIOL (2R,3R)
An impurity of Efinaconazole, a triazole antifungal approved to treat fungal infections of the toenails as a topical solution. Grade: 95%. CAS No. 135133-23-2. Molecular formula: C17H21F2N3O3. Mole weight: 353.36.
Eflornithine hydrochloride
Eflornithine hydrochloride is a drug found to be effective in the treatment of facial hirsutism. It is a "suicide inhibitor," irreversibly binding to Ornithine Decarboxylase (ODC) and preventing the natural substrate ornithine from accessing the active site. Synonyms: DFMO hydrochloride; MDL71782 hydrochloride; RMI71782 hydrochloride; MDL 71782 hydrochloride; RMI 71782 hydrochloride; MDL-71782 hydrochloride; RMI-71782 hydrochloride; α-difluoromethylornithine hydrochloride; Vaniqa hydrochloride. Grade: >98%. CAS No. 68278-23-9. Molecular formula: C6H13ClF2N2O2. Mole weight: 218.63.
Efloxate
Efloxate, a flavone derivative, could be effective in the treatment of chronic coronary insufficiency and angina pectoris for acting as a vasodilator. Uses: Efloxate could be effective in the treatment of chronic coronary insufficiency and angina pectoris for acting as a vasodilator. Synonyms: RE 1-0185; RE-1-0185; RE1-0185; efloxate; EFLOXATE/EFLOXATEM; Corosamin; Domucor; Eflocor; Oxyflavyl; Recordil; 2-(4-keto-2-phenyl-chromen-7-yl)oxyacetic acid ethyl ester. Grade: 98%. CAS No. 119-41-5. Molecular formula: C19H16O5. Mole weight: 324.33.
EFONIDIPINE
Efonidipine could be effective in the treatment of cardiovascular disease as a blocker of T-type and L-type calcium channels. It could also present as the hydrochloride salt form. Uses: Efonidipine could be effective in the treatment of cardiovascular disease as a blocker of t-type and l-type calcium channels. Synonyms: NZ-105; NZ 105; NZ105; Efonidipine; Efonidipine[INN]; 111011-63-3; C34H38N3O7P; Efonidipine(INN); Landel. Grade: 95%. CAS No. 111011-63-3. Molecular formula: C34H38N3O7P. Mole weight: 631.66.
EFONIDIPINE HCL
The hydrochloride salt form of Efonidipine which could be effective in the treatment of cardiovascular disease as a blocker of T-type and L-type calcium channels. Uses: The hydrochloride salt form of efonidipine which could be effective in the treatment of cardiovascular disease as a blocker of t-type and l-type calcium channels. Synonyms: EFONIDIPINE HCL; Efonidipine hydrochloride. Grade: 95%. CAS No. 111011-53-1. Molecular formula: C34H38N3O7P.HCl. Mole weight: 668.12.
Efonidipine hydrochloride monoethanolate
The hydrochloride monoethanolate salt form of Efonidipine which has been launched for hypertension and discontinued for cerebrovascular disorders. Uses: The hydrochloride monoethanolate salt form of efonidipine which has been launched for hypertension and discontinued for cerebrovascular disorders. Synonyms: Efonidipine hydrochloride ethanol; Efonidipine hydrochloride ethanolate; NZ 105 ethanolate; NZ105 ethanolate; NZ-105 ethanolate; EFONIDIPINE HYDROCHLORIDE MONOETHANOLATE; 111011-76-8; Efonidipine.HCl ethanolate. Grade: >98%. CAS No. 111011-76-8. Molecular formula: C36H45ClN3O8P. Mole weight: 631.66.
eFT-508
eFT-508 is a selective inhibitor of MNK1/2 (IC50s = 2.4 nM and 1 nM respectively) inhibiting MNK1/2-mediated signaling and the phosphorylation of certain regulatory proteins. It acts against tumor. Synonyms: SCHEMBL17362622; AKOS030627405; ZINC575623807; CS-5841; CS 5841; CS5841; 6-[(6-aminopyrimidin-4-yl)amino]-8-methylspiro[2H-imidazo[1,5-a]pyridine-3,1'-cyclohexane]-1,5-dione; eFT508. Grade: 98%. CAS No. 1849590-01-7. Molecular formula: C17H20N6O2. Mole weight: 340.38.
Efungumab
Efungumab is a human recombinant monoclonal antibody with antifungal activity. Efungumab binds to HSP 90, preventing a conformational change needed for fungal viability. Efungumab has the potential for the treatment of invasive candidiasis. Grade: 95%. CAS No. 762260-74-2.
EG 00229
EG 00229 is a neuropilin 1 (NRP1) receptor antagonist, inhibiting VEGFA binding to the NRP1 b1 domain. Synonyms: EG00229; EG-00229; EG 00229; N2-[[3-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-2-thienyl]carbonyl]-L-arginine. Grade: ≥98% by HPLC. CAS No. 1018927-63-3. Molecular formula: C17H19N7O5S3. Mole weight: 497.57.
EG 00229 Trifluoroacetate
EG00229 is a small molecule inhibitor of neuropilin-1(Nrp1) with an IC50 of 3μM. EG00229 has been reported to inhibit VEGF-A binding to PAE/NRP1 in the Nrp1and bt-VEGF-A binding to purified Nrp1 b1 domain in a cell-free assay with an IC50 value of 8μM and 3μM, respectively. In addition, EG00229 has also shown the inhibition of VEGF-A binding to VEGFR2, VEGFR1 and Nrp1 in human umbilical vein endothelial cells (HUVECs) in a dose-dependent manner with an IC50 value of 23μM [1]. Besides, EG00229 has been revealed to prevent tuftsin binding to the Nrp1 which is at the cell surface. Moreover, EG00229 has been noted to suppress the anti-inflammatory M2 shift in microglia induced by tuftsin and thus potently prevent tuftsin's action. Synonyms: EG 00229; EG-00229. Grade: >98%. CAS No. 1210945-69-9. Molecular formula: C19H20F3N7O7S3. Mole weight: 611.6.
EG01377
EG01377 is a potent, bioavailable and selective neuropilin-1 (NRP1) inhibitor, with a Kd of 1.32 μM, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1. It has antiangiogenic, antimigratory and antitumor effects. Synonyms: (3-((5-(4-(aminomethyl)phenyl)-2,3-dihydrobenzofuran)-7-sulfonamido)thiophene-2-carbonyl)-L-arginine; N2-({3-[({5-[4-(Aminomethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl}sulfonyl)amino]-2-thienyl}carbonyl)-N5-(diaminomethylene)-L-ornithine. Grade: ≥98%. CAS No. 2227996-00-9. Molecular formula: C26H30N6O6S2. Mole weight: 586.68.
EG01377 dihydrochloride
EG01377 dihydrochloride is a potent, bioavailable and selective neuropilin-1 (NRP1) inhibitor, with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. It has antiangiogenic, antimigratory and antitumor effects. Synonyms: N2-({3-[({5-[4-(Aminomethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl}sulfonyl)amino]-2-thienyl}carbonyl)-N5-(diaminomethylene)-L-ornithine dihydrochloride; L-Ornithine, N2-[[3-[[[5-[4-(aminomethyl)phenyl]-2,3-dihydro-7-benzofuranyl]sulfonyl]amino]-2-thienyl]carbonyl]-N5-(diaminomethylene)-, hydrochloride (1:2). Grade: ≥98%. Molecular formula: C26H32Cl2N6O6S2. Mole weight: 659.60.
EG1
EG1 is a specific inhibitor of specific Paired box 2 (Pax2), which targets the DNA binding domain and inhibits embryonic kidney development. CAS No. 693241-54-2. Molecular formula: C22H18N2O5. Mole weight: 390.39.
Eg5-I
Eg5, also known as KSP and Kif11, is a kinesin-like spindle protein that is essential for establishing a bipolar spindle during mitosis. Eg5-I is a potent inhibitor of Eg5, both in vitro and in cells (IC50s = 127 and 190 nM, respectively). Synonyms: (2R)-2-amino-3-[[(4-methoxyphenyl)diphenylmethyl]thio]-1-propanol. Grade: ≥98%. CAS No. 1338701-15-7. Molecular formula: C23H25NO2S. Mole weight: 379.5.
Eg5 Inhibitor V, trans-24
Eg5 Inhibitor V, trans-24 is a potent and specific inhibitor of kinesin Eg5 with an IC50 of 0.65 μM. It can be used in cancer research. Synonyms: 1H-Imidazo[1',5':1,6]pyrido[3,4-b]indole-1,3(2H)-dione, 5,6,11,11a-tetrahydro-5-(3-hydroxyphenyl)-2-(phenylmethyl)-, (5R,11aS)-; (5R,11aS)-2-Benzyl-5-(3-hydroxyphenyl)-5,6,11,11a-tetrahydro-1H-imidazo[1',5':1,6]pyrido[3,4-b]indole-1,3(2H)-dione; Trans-24. Grade: ≥95%. CAS No. 869304-55-2. Molecular formula: C26H21N3O3. Mole weight: 423.46.
EGA
EGA is an inhibitor of endosomal trafficking. EGA is a small molecule that blocks the entry of anthrax lethal toxin by inhibiting trafficking pathways in acidified endosomes, without affecting endosome pH. It also blocks trafficking of other toxins, except ricin. Synonyms: 2-[(4-bromophenyl)methylene]-N-(2,6-dimethylphenyl)-hydrazinecarboxamide. Grade: ≥98%. CAS No. 415687-81-9. Molecular formula: C16H16BrN3O. Mole weight: 346.2.
EGF816
EGF816, also called as Nazartinib, a covalent mutant-selective EGFR inhibitor and potently inhibits the T790M resistance mutation while sparing wild-type EGFR. in vivo: demonstrated strong tumor regressions in several EGFR activating and resistant tumor m. Synonyms: EGF816; EGF-816; EGF 816; NVS-816; NVS 816; NVS816; Nazartinib; N-[7-chloro-1-[(3R)-1-[(E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]benzimidazol-2-yl]-2-methylpyridine-4-carboxamideEGF816UNII-KE7K32EME8KE7K32EME8EGF-8161508250-71-2GTPL9204SCHEMBL16767232SCHEMBL16767240EGF 816compound 47 [PMID: 27433829]. CAS No. 1508250-71-2. Molecular formula: C26H31ClN6O2. Mole weight: 495.02.
EGF816 mesylate
EGF816 mesylate is the mesylate salt of EGF816 which is a covalent mutant-selective EGFR inhibitor and potently inhibits the T790M. Synonyms: N-[7-chloro-1-[(3R)-1-[(E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]benzimidazol-2-yl]-2-methylpyridine-4-carboxamide; methanesulfonic acid. CAS No. 1508250-72-3. Molecular formula: C27H35ClN6O5S. Mole weight: 591.12.
EGFR/CSC-IN-1
EGFR/CSC-IN-1 is a potential dual inhibitor of EGFR and cancer stem cell (CSC) with an IC50 of 10.52 nM for EGFR. It is used to treat triple negative breast cancer. Synonyms: 2-(4-(3-(2-chloro-10H-phenothiazin-10-yl)propyl)piperazin-1-yl)ethyl 4-(((5-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)furan-2-yl)methyl)(2-(methylsulfonyl)ethyl)amino)-4-oxobutanoate. Molecular formula: C54H54Cl2FN7O7S2. Mole weight: 1067.08.
EGFR/ErbB2 Inhibitor
EGFR/ErbB2 inhibitor is a cell-permeable 4-anilino quinazoline compound, which is a potent and reversible inhibitor of EGFR and c-ErbB2 (IC50s = 20 and 79 nM, respectively). It inhibits the proliferation of cancer cells overexpressing either c-ErbB2 or EGFR (IC50s = 2.3-2.5 μM). Synonyms: 4557W; 4-(4-Benzyloxyanilino)-6,7-dimethoxyquinazoline; EGFR/ErbB-2 Inhibitor. Grade: ≥95%. CAS No. 179248-61-4. Molecular formula: C23H21N3O3. Mole weight: 387.4.
EGFR-IN-1
EGFR-IN-1 is an orally active and irreversible mutant selective EGFR inhibitor of L858R/T790M that effectively inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. It shows strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. It has antitumor activity. Synonyms: N-{3-[2-({4-[2-(Dimethylamino)ethoxy]-2-methoxyphenyl}amino)-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]phenyl}acrylamide; 2-Propenamide, N-[3-[2-[[4-[2-(dimethylamino)ethoxy]-2-methoxyphenyl]amino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]phenyl]-. Grade: ≥95%. CAS No. 1625677-63-5. Molecular formula: C28H30N6O4. Mole weight: 514.58.
EGFR-IN-11
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM against the triple mutant EGFRL858R/T790M/C797S. It significantly inhibits EGFR phosphorylation, induces apoptosis and arrests cell cycle at G0/G1. Synonyms: 9H-Purine-2,8-diamine, 9-[(3R)-1-(cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl-; 9-[(3R)-1-(Cyclopropylsulfonyl)-3-pyrrolidinyl]-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-phenyl-9H-purine-2,8-diamine. Grade: ≥95%. CAS No. 2463200-44-2. Molecular formula: C29H35N9O2S. Mole weight: 573.71.
EGFR-IN-15
EGFR-IN-15, an EGFR inhibitor with an IC50 of 4 nM, can be used in the study of oncological disease. Synonyms: 1H,10H-4,8-Metheno-17H-pyrazolo[3',4':2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9-one, 14-bromo-18,19,20,21-tetrahydro-1,6,18-trimethyl-, (18R)-. CAS No. 2573869-16-4. Molecular formula: C24H25BrN6O2. Mole weight: 509.40.
EGFR-IN-16
EGFR-IN-16 is a potent inhibitor of EGFR with pIC50 of 4.85 and 4.74 for EGFR and HER-2, respectively. Synonyms: Benzenepropanenitrile, α-[(3,4-dihydroxyphenyl)methylene]-β-oxo-, (αE)-; (E)-2-Benzoyl-3-(3,4-dihydroxyphenyl)acrylonitrile; (2E)-2-benzoyl-3-(3,4-dihydroxyphenyl)prop-2-enenitrile; (2E)-2-Benzoyl-3-(3,4-dihydroxyphenyl)acrylonitrile. Grade: ≥95%. CAS No. 133550-22-8. Molecular formula: C16H11NO3. Mole weight: 265.26.
EGFR-IN-17
EGFR-IN-17 is a potent and selective epidermal growth factor receptor inhibitor (IC50 = 0.0002 μM) that overcomes C797S-mediated resistance. Synonyms: (2-((5-chloro-2-((2-methoxy-5-(1-methyl-1H-pyrazol-4-yl)-4-morpholinophenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide. Molecular formula: C27H31ClN7O3P. Mole weight: 568.01.
EGFR-IN-18
EGFR-IN-18 effectively inhibits enzymatic activity in L858R/T790M/C797S mutant EGFR, but has a significantly lower activity for wild-type EGFR. Synonyms: N-[3-[5-(2-acetamidopyridin-4-yl)-2-methylsulfanyl-1H-imidazol-4-yl]phenyl]-2-[(3-oxo-1H-isoindol-2-yl)methyl]benzamide; N-(3-{5-[2-(acetylamino)pyridin-4-yl]-2-(methylsulfanyl)-1H-imidazol-4-yl}phenyl)-2-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]benzamide; TQA. Molecular formula: C33H28N6O3S. Mole weight: 588.68.
EGFR-IN-1 hydrochloride
EGFR-IN-1 hydrochloride is an orally active and irreversible mutant selective EGFR inhibitor of L858R/T790M that effectively inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. It shows strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. It has antitumor activity. Synonyms: N-{3-[2-({4-[2-(Dimethylamino)ethoxy]-2-methoxyphenyl}amino)-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]phenyl}acrylamide hydrochloride (1:1); 2-Propenamide, N-[3-[2-[[4-[2-(dimethylamino)ethoxy]-2-methoxyphenyl]amino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]phenyl]-, hydrochloride (1:1). Grade: ≥95%. CAS No. 2227455-78-7. Molecular formula: C28H31ClN6O4. Mole weight: 551.04.
EGFR-IN-1 TFA
EGFR-IN-1 TFA is an orally active and irreversible mutant selective EGFR inhibitor of L858R/T790M that effectively inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. It shows strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. It has antitumor activity. Synonyms: N-{3-[2-({4-[2-(Dimethylamino)ethoxy]-2-methoxyphenyl}amino)-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]phenyl}acrylamide trifluoroacetate (1:1); Acetic acid, 2,2,2-trifluoro-, compd. with N-[3-[2-[[4-[2-(dimethylamino)ethoxy]-2-methoxyphenyl]amino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]phenyl]-2-propenamide (1:1). Grade: ≥99%. Molecular formula: C30H31F3N6O6. Mole weight: 628.60.
EGFR-IN-2
EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor. It showed excellent cellular activity against both the single and double mutants of EGFR, demonstrating target engagement in vivo and ADME-PK properties that are suitable for further evaluation. CAS No. 1643497-70-4. Molecular formula: C26H33N9O3S. Mole weight: 551.66.
EGFR-IN-5
EGFR-IN-5 is an inhibitor of EGFR with IC50s of 10.4, 1.1, 34 and 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M and EGFRL858R/T790M/C797S, respectively. Synonyms: mutant EGFR inhibitor B30; (1-(6-((5-(4-(Dimethylamino)piperidin-1-yl)pyridin-2-yl)amino)-2-((4-fluorophenyl)amino)pyrido[3,4-d]pyrimidin-4-yl)piperidin-4-yl)methanol; 4-Piperidinemethanol, 1-[6-[[5-[4-(dimethylamino)-1-piperidinyl]-2-pyridinyl]amino]-2-[(4-fluorophenyl)amino]pyrido[3,4-d]pyrimidin-4-yl]-. Grade: ≥95%. CAS No. 2225887-26-1. Molecular formula: C31H38FN9O. Mole weight: 571.69.
EGFR-IN-7
EGFR-IN-7 is a selective and potent EGFR kinase inhibitor. TQB3804 displays potent enzymatic activities for EGFRd746-750/T790M/C797S, EGFRL858R/T790M/C797S, EGFRd746-750/T790M, and EGFRL858R/T790M with IC50 of 0.46, 0.13, 0.26, and 0.19 nM, respectively. Synonyms: TQB3804. CAS No. 2267329-76-8. Molecular formula: C32H41BrN9O2P. Mole weight: 694.60.
EGFR-IN-8
EGFR-IN-8, a dual inhibitor of EGFR and c-Met, may be a promising candidate for further development to target EGFR TKI-resistant NSCLC. Synonyms: N-(3-Chloro-4-(5-(3-(3-(4-(cyclopropanecarboxamido)-3-(trifluoromethyl)phenyl)ureido)phenyl)-1,2,4-oxadiazol-3-yl)phenyl)nicotinamide; N-(3-chloro-4-{5-[3-({[4-cyclopropaneamido-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenyl]-1,2,4-oxadiazol-3-yl}phenyl)pyridine-3-carboxamide; 3-Pyridinecarboxamide, N-[3-chloro-4-[5-[3-[[[[4-[(cyclopropylcarbonyl)amino]-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]phenyl]-1,2,4-oxadiazol-3-yl]phenyl]-. Grade: ≥98%. CAS No. 2407957-87-1. Molecular formula: C32H23ClF3N7O4. Mole weight: 662.02.
EGFR-IN-9
EGFR-IN-9 is a potent inhibitor of EGFR kinase with IC50s of 7 and 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). It has antitumor activity. Synonyms: (S)-N-(3-(4-(2-hydroxy-1-phenylethylamino)-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl)acrylamide; 2-Propenamide, N-[3-[4-[[(1S)-2-hydroxy-1-phenylethyl]amino]-6-phenylfuro[2,3-d]pyrimidin-5-yl]phenyl]-. Grade: ≥95%. CAS No. 1226549-39-8. Molecular formula: C29H24N4O3. Mole weight: 476.53.
EGFR Inhibitor
A cell-permeable and highly selective EGFR tyrosine kinase inhibitor with IC50 value in the nanomolar range. Inhibition of EGFR induces apoptosis of tumor cells by ownregulating antiapoptotic proteins such as survivin and upregulating proapoptotic proteins such as Bim. Uses: Antitumor agent. Synonyms: EGFR inhibitor; EGFR-inhibitor; EGFRinhibitor; Cyclopropanecarboxylic acid-(3-(6-(3-trifluoromethyl-phenylamino)-pyrimidin-4-ylamino)-phenyl)-amide; N-(3-((6-((3-(Trifluoromethyl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)cyclopropanecarboxamide; K00598a. Grade: 99%. CAS No. 879127-07-8. Molecular formula: C21H18F3N5O. Mole weight: 413.4.
EGFR mutant-IN-1
EGFR mutant-IN-1 is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor (IC50 = 27.5 nM), and a significantly less potent for EGFRWT (IC50 >1.0 μM). Synonyms: 6-(2-Chloro-3-fluorophenyl)-5-methyl-2-{[3-methyl-4-(4-methyl-1-piperazinyl)phenyl]amino}-8-[(3R)-1-propionyl-3-piperidinyl]pyrido[2,3-d]pyrimidin-7(8H)-one; Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-(2-chloro-3-fluorophenyl)-5-methyl-2-[[3-methyl-4-(4-methyl-1-piperazinyl)phenyl]amino]-8-[(3R)-1-(1-oxopropyl)-3-piperidinyl]-. Molecular formula: C34H39ClFN7O2. Mole weight: 632.17.
Eggmanone
Eggmanone is a potent and selective phosphodiesterase (PDE) 4 inhibitor (IC50 = 72 nM) displaying >40-fold selectivity over PDE3, PDE10, and PDE11. Eggmanone acts via blocking hedgehog signaling through PDE antagonism, downstream of smoothened signaling. Synonyms: 5,6,7,8-Tetrahydro-3-(2-methyl-2-propen-1-yl)-2-[[2-oxo-2-(2-thienyl)ethyl]thio]-[1]benzothieno[2,3-d]pyrimidin-4(3H)-one. Grade: ≥98% by HPLC. CAS No. 505068-32-6. Molecular formula: C20H20N2O2S3. Mole weight: 416.58.
EGIS-8332
EGIS-8332 potently decreased AMPA and quisqualate induced LDH release (IC50 = 5.2 ± 0.4 and 7.4 ± 1.3 μM, respectively) from the cells. The inhibition of the AMPA/kainate ion channels by EGIS-8332 is non-competitive, not use dependent, and depends neither on the closed/open state of the channel, nor the membrane potential. Synonyms: 7-acetyl-5-(4-aminophenyl)-8-methyl-9H-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-8-carbonitrile; EGIS-8332; EGIS 8332; EGIS8332. Grade: >98%. CAS No. 220725-87-1. Molecular formula: C20H18N4O3. Mole weight: 362.389.
EGLU
EGLU is a group II mGluR antagonist and also a selective antagonist of presynaptically-mediated (1S,3S)-ACPD-induced depression of motoneuron excitation in neonatal rat spinal cord. Synonyms: (2S)-α-Ethylglutamic acid; (2S)-2-amino-2-ethylpentanedioic acid. Grade: ≥95% by HPLC. CAS No. 170984-72-2. Molecular formula: C7H13NO4. Mole weight: 175.18.
EGT1442
EGT1442 is a potent and selective SGLT2 inhibitor with IC50 value of 5.6 μM /2 nM in SGLT1 /SGLT2 respectively. It significantly prolonged the median survival of SHRSP rats. It attenuates blood glucose and HbA(1c) levels and prolongs the survival of stroke-prone rats in db/db mice. It showed favorable properties both in vitro and in vivo and could be beneficial to the management of type 2 diabetic patients. It was developed by Theracos and in clinic phase 1 trials. Uses: Egt1442 showed favorable properties and could be beneficial to the management of type 2 diabetic patients. Synonyms: THR1442; THR-1442; THR 1442; EGT1442; EGT-1442; EGT 1442; Bexagliflozin; (1S)-1,5-Anhydro-1-C-[4-chloro-3-[[4-[2-(cyclopropyloxy)ethoxy]phenyl]methyl]phenyl]-D-glucitol; Bexagliflozin; THR1442; EGT0001442; EGT-1442; THR-1442; EGT-0001442; (2S,4R,6R)-2-(4-chloro-3-(4-(2-cyclopropoxyethoxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol; (3R,4R,5S,6R)-2-(4-chloro-3-(4-(2-cyclopropoxyethoxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol. Grade: >98%. CAS No. 1118567-05-7. Molecular formula: C24H29ClO7. Mole weight: 464.94.
EHMT2-IN-1
EHMT2-IN-1 is a potent inhibitor of EHMT, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. It is used for the study of blood disorder or cancer. Synonyms: N2-(4-Methoxy-3-{4-[(methylamino)methyl]-1H-pyrazol-1-yl}phenyl)-N4,6-dimethyl-2,4-pyrimidinediamine; 2,4-Pyrimidinediamine, N2-[4-methoxy-3-[4-[(methylamino)methyl]-1H-pyrazol-1-yl]phenyl]-N4,6-dimethyl-. Grade: ≥97%. CAS No. 2230849-55-3. Molecular formula: C18H23N7O. Mole weight: 353.42.
EHMT2-IN-2
EHMT2-IN-2 is a potent inhibitor of EHMT, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. It is used for the study of blood disorder or cancer. Synonyms: EHMT2 inhibitor 2; 2,4-Pyrimidinediamine, N2-[4-methoxy-3-(3-methyl-1H-pyrrolo[2,3-c]pyridin-2-yl)phenyl]-N4,6-dimethyl-; N2-[4-Methoxy-3-(3-methyl-1H-pyrrolo[2,3-c]pyridin-2-yl)phenyl]-N4,6-dimethyl-2,4-pyrimidinediamine. Grade: ≥95%. CAS No. 2230850-47-0. Molecular formula: C21H22N6O. Mole weight: 374.44.
EHNA hydrochloride
EHNA hydrochloride is a selective inhibitor of cGMP-stimulated phosphodiesterase (PDE2) (IC50 = 0.8 - 4 μM) and also an inhibitor of adenosine deaminase. EHNA inhibits spontaneous differentiation of human ESCs in feeder-free conditions and directed neuronal differentiation. Uses: Antiviral agents. Synonyms: (2S,3R)-3-(6-aminopurin-9-yl)nonan-2-ol hydrochloride. Grade: >98%. CAS No. 58337-38-5. Molecular formula: C14H23N5O.HCl. Mole weight: 313.83.
EHop-016
EHop-016 is a rac GTPase inhibitor that blocks the interaction of Rac with GEF Vav in metastatic human breast cancer cells. Synonyms: N4-(9-Ethyl-9H-carbazol-3-yl)-N2-(3-morpholinopropyl)pyrimidine-2,4-diamine; N4-(9-Ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]-2,4-pyrimidinediamine. Grade: 98%. CAS No. 1380432-32-5. Molecular formula: C25H30N6O. Mole weight: 430.5.
EHP-101
EHP-101 is an orally active, specific PPARγ and CB2 receptor dual agonist that inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. HP-101 is a semi-synthetic multi-target cannabinoquinoid with potent anti-inflammatory activity. It attenuates adipogenesis and prevents diet-induced obesity. Synonyms: VCE-004.8; (1'R,6'R)-3-(benzylamino)-6-hydroxy-3'-methyl-4-pentyl-6'-(prop-1-en-2-yl)-[1,1'-bi(cyclohexane)]-2',3,6-triene-2,5-dione; 2,5-Cyclohexadiene-1,4-dione, 2-hydroxy-3-((1R,6R)-3-methyl-6-(1-methylethenyl)-2-cyclohexen-1-yl)-6-pentyl-5-((phenylmethyl)amino)-; (1'R,6'R)-3-(Benzylamino)-6-hydroxy-6'-isopropenyl-3'-methyl-4-pentyl-1,1'-bi(cyclohexane)-2',3,6-triene-2,5-dione. Grade: ≥98%. CAS No. 1818428-24-8. Molecular formula: C28H35NO3. Mole weight: 433.58.
Ehp-inhibitor-1
Ehp-inhibitor-1 is an Eph family tyrosine kinase inhibitor targeting Eph receptors. Study indicated that inhibition of Eph receptors results in an increase in glucose-stimulated insulin secretion from mouse and human pancreatic islets. Synonyms: 6-(3-methoxyphenyl)-3-pyridin-3-ylpyrazolo[1,5-a]pyrimidin-7-amine. CAS No. 861249-59-4. Molecular formula: C18H15N5O. Mole weight: 317.352.
Ehp-inhibitor-2
Ehp-inhibitor-2 is an Eph family tyrosine kinase inhibitor targeting Eph receptors. Study indicated that inhibition of Eph receptors results in an increase in glucose-stimulated insulin secretion from mouse and human pancreatic islets. Synonyms: 3-(7-amino-3-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidin-6-yl)phenol. CAS No. 861249-77-6. Molecular formula: C17H13N5O. Mole weight: 303.325.
EHT 1864
EHT 1864 is a potent Rac family GTPase inhibitor with Kd of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. Synonyms: EHT 1864; EHT1864; EHT-1864. Grade: >98%. CAS No. 754240-09-0. Molecular formula: C25H29Cl2F3N2O4S. Mole weight: 581.47.
EHT 5372
EHT 5372 is a selective and highly potent inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44 and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α and GSK-3β, respectively. Synonyms: Methyl 9-[(2,4-dichlorophenyl)amino][1,3]thiazolo[5,4-f]quinazoline-2-carboximidate; Thiazolo[5,4-f]quinazoline-2-carboximidic acid, 9-[(2,4-dichlorophenyl)amino]-, methyl ester. Grade: ≥95%. CAS No. 1425945-63-6. Molecular formula: C17H11Cl2N5OS. Mole weight: 404.27.
EHT-6706
EHT-6706 is a novel microtubule-disrupting agent that targets the colchicine-binding site to inhibit tubulin polymerization. At low nM concentrations, EHT 6706 exhibits highly potent antiproliferative activity on more than 60 human tumor cell lines, even those described as being drug resistant. EHT 6706 also shows strong efficacy as a vascular-disrupting agent, since it prevents endothelial cell tube formation and disrupts pre-established vessels, changes the permeability of endothelial cell monolayers and inhibits endothelial cell migration. Genome-wide transcriptomic analysis of EHT 6706 effects on human endothelial cells shows that the antiangiogenic activity elicits gene deregulations of antiangiogenic pathways. These findings indicate that EHT 6706 is a promising tubulin-binding compound with potentially broad clinical antitumor efficacy. Synonyms: EHT6706; EHT 6706; EHT-6706. CAS No. 1351592-10-3. Molecular formula: C21H24N2O4. Mole weight: 368.43.
EHT-6706 dihydrochloride
EHT-6706 can target the colchicine-binding site to inhibit tubulin polymerization as a tubulin polymerisation inhibitor. It is under the development of Diaxonhit. EHT 6706 also is a vascular-disrupting agent. It can prevent endothelial cell tube formation and disrupt pre-established vessels, change the permeability of endothelial cell monolayers and inhibit endothelial cell migration. In Jul 2013, preclincal development for treatment of cancer was ongoing in the USA. Uses: Cancer. Synonyms: EHT-6706 dihydrochloride; EHT 6706 dihydrochloride; EHT6706 dihydrochloride; 7-ethoxy-4-(3,4,5-trimethoxybenzyl)isoquinolin-8-amine dihydrochloride. Grade: 98%. CAS No. 1351592-09-0. Molecular formula: C21H26Cl2N2O4. Mole weight: 441.35.