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Mutant IDH1-IN-1, a mutant IDH1 R132H inhibitor, could be used in some biological studies. Uses: Mutant idh1-in-1 is a mutant idh1 r132h inhibitor that could be used in some biological studies. Synonyms: Mutant IDH1-IN-1; 1355326-21-4; MutantIDH1-IN-1; IDH1-IN-1; SCHEMBL15118896; C30H31FN4O2. Grades: 98%. CAS No. 1355326-21-4. Molecular formula: C30H31FN4O2. Mole weight: 498.59.
Mutant IDH1-IN-2
Mutant IDH1-IN-2, aslo called as SCHEMBL14831158, is an inhibitor of mutant IDH protein. It is developed for the treatment of diseases associated with such mutant IDH proteins, such as cancer. Synonyms: (4S) -3-[2-[[ (1S) -1-[4-[ (4, 4-difluoropiperidin-1-yl) methyl]phenyl]ethyl]amino]pyrimidin-4-yl]-4-propan-2-yl-1, 3-oxazolidin-2-oneMutant IDH1-IN-2 SCHEMBL14831158 BDBM146172 CS-5119 HY-18717 US8957068, 224 (S)-3-(2-(((S)-1-(4-((4,4-difluoropiperidin-1-yl)met. CAS No. 1429176-69-1. Molecular formula: C24H31F2N5O2. Mole weight: 459.53.
Mutant IDH1 inhibitor
Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC 50 of < 72 nM. Uses: Scientific research. Group: Signaling pathways. CAS No. 1429180-08-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13972.
2-Aminotetraline-2-carboxylic acid
2-Aminotetraline-2-carboxylic acid is a potent and selective IDH1 (isocitrate dehydrogenase 1) mutant inhibitor for the treatment of acute myeloid leukemia. Synonyms: Atc-OH; 2-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid; 2-Aminotetralin-2-carboxylic acid; D,L-2-Aminotetralin-2-carboxylic acid; 2-AMINOTETRALINE-2-CARBOXYLIC ACID; 2-Amino-1,2,3,4-tetrahydro-2-naphthalenecarboxylicacid; 2-amino-3,4-dihydro-1H-naphthalene-2-carboxylic acid; (R)-2-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid; (+/-)-2-Amino-1,2,3,4-tetrahydro-2-naphthoic acid; GSK 321; Atc OH. Grades: ≥ 98% (HPLC). CAS No. 6331-63-1. Molecular formula: C11H13NO2. Mole weight: 191.22.
AGI-5198
AGI-5198, also know as IDH-C35, is the a very potent and selective mutant IDH1 inhibitor that was shown to potential anticancer activity. AGI-5198 shows good potency in the U87 R132H cell based assay and ~90% tumor 2-HG inhibition in the corresponding mouse xenograft model following BID dosing. AGI-5198 inhibits IDH1 R132H mutant and R132C mutant in vitro with IC50 ~0.07 μM and ~0.16 μM, respectively. Uses: Designed for use in research and industrial production. Additional or Alternative Names: AGI5198; AGI-5198; AGI 5198; IDHC35; IDH-C35; IDH C35. Product Category: Inhibitors. Appearance: White to off-white solid powder. CAS No. 1355326-35-0. Molecular formula: C27H31FN4O2. Mole weight: 462.56. Purity: >98%. IUPACName: N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-(o-tolyl)acetamide. Canonical SMILES: O=C(NC1CCCCC1)C(N(C2=CC=CC(F)=C2)C(CN3C=CN=C3C)=O)C4=CC=CC=C4C. Product ID: ACM1355326350. Alfa Chemistry ISO 9001:2015 Certified.
AGI-5198
AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM. Synonyms: AGI5198; AGI-5198; AGI 5198; IDHC35; IDH-C35; IDH C35. Grades: >98%. CAS No. 1355326-35-0. Molecular formula: C27H31FN4O2. Mole weight: 462.56.
AGI-6780
AGI-6780 is an IDH2 inhibitor that potently and selectively inhibits the tumor-associated mutant IDH2/R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2WT with IC50of 190±8.1 nM. Synonyms: AGI6780; AGI 6780; AGI-6780. CAS No. 1432660-47-3. Molecular formula: C21H18F3N3O3S2. Mole weight: 481.508.
alpha-Mangostin
alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 ( IDH1-R132H ) with a K i of 2.85 μM. Uses: Scientific research. Group: Natural products. Alternative Names: α-Mangostin. CAS No. 6147-11-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-N0328.
Alpha-Mangostin
Alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. Uses: Designed for use in research and industrial production. Additional or Alternative Names: Α-Mangostin. Product Category: Inhibitors. Appearance: Solid. CAS No. 6147-11-1. Molecular formula: C24H26O6. Mole weight: 410.46. Purity: 0.9964. Canonical SMILES: O=C1C2=C(OC3=C1C(C/C=C(C)\C)=C(OC)C(O)=C3)C=C(O)C(C/C=C(C)\C)=C2O. Product ID: ACM6147111-1. Alfa Chemistry ISO 9001:2015 Certified.
alpha-Mangostin (Standard)
alpha-Mangostin (Standard) is the analytical standard of alpha-Mangostin. This product is intended for research and analytical applications. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 ( IDH1-R132H ) with a K i of 2.85 μM. Uses: Scientific research. Group: Natural products. Alternative Names: α-Mangostin (Standard). CAS No. 6147-11-1. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-N0328R.
BAY 1436032
BAY-1436032 is a highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). It is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displays potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants. BAY 1436032 strongly reduces 2-HG (2-hydroxyglutarate) levels in cells carrying IDH1-R132H, -R132C, -R132G, -R132S and -R132L mutations. BAY 1436032 showed a favourable selectivity profile against wtIDH1/2 and a large panel of off-targets in vitro. Synonyms: 3-(2-[[4-(Trifluoromethoxy)phenyl]amino]-1-[(1R,5R)-3,3,5-trimethylcyclohexyl]-1H-benzimidazol-5-yl)propanoic Acid; BAY-1436032. Grades: ≥98%. CAS No. 1803274-65-8. Molecular formula: C26H30F3N3O3. Mole weight: 489.53.
BAY-1436032
BAY-1436032 is a potent, selective and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). BAY 1436032 is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displayed potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants. In line with the proposed mode of action, a concentration-dependent lowering of 2-HG was observed in vitro accompanied by differentiation and maturation of mIDH1 tumor cells. Furthermore, BAY 1436032 showed a favourable selectivity profile against wtIDH1/2 and a large panel of off-targets in vitro. Uses: Designed for use in research and industrial production. Additional or Alternative Names: BAY-1436032; BAY 1436032; BAY1436032. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 1803274-65-8. Molecular formula: C26H30F3N3O3. Mole weight: 489.54. Purity: >98%. IUPACName: 3-(2-((4-(trifluoromethoxy)phenyl)amino)-1-((1R,5R)-3,3,5-trimethylcyclohexyl)-1H-benzo[d]imidazol-5-yl)propanoic acid. Canonical SMILES: O=C(O)CCC1=CC=C2N([C@H]3CC(C)(C)C[C@@H](C)C3)C(NC4=CC=C(OC(F)(F)F)C=C4)=NC2=C1. Product ID: ACM1803274658. Alfa Chemistry ISO 9001:2015 Certified.
Crelosidenib
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC 50 s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H , IDH1 R132C , IDH2 R140Q and IDH2 R172K mutant enzymes , respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: LY3410738; Mutant IDH1-IN-6. CAS No. 2230263-60-0. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-131312.
Enasidenib
Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC 50 s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K , respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AG-221. CAS No. 1446502-11-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-18690.
Enasidenib mesylate
Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes indicated for the treatment of adult patients with replased or refractory acute myeloid leukemia (AML) with an isocitrate dehydrogenase-2 (IDH2) mutation. Synonyms: methanesulfonic acid;2-methyl-1-[[4-[6-(trifluoromethyl)pyridin-2-yl]-6-[[2-(trifluoromethyl)pyridin-4-yl]amino]-1,3,5-triazin-2-yl]amino]propan-2-ol; Enasidenib (mesylate); AG-221 mesylate; Enasidenib mesilate; Enasidenib methanesulfonate; Enasidenib mesylate [USAN]. CAS No. 1650550-25-6. Molecular formula: C20H21F6N7O4S. Mole weight: 569.48.
Enasidenib mesylate
Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AG-221 mesylate. CAS No. 1650550-25-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-18690A.
GSK321
GSK321 is a highly potent, selective inhibitor of mutant IDH1 enzymes, with IC50=4.6 nM against R132H, 3.8 nM against R132C and 2.9 nM against R132G. GSK321 stably decreased 2-hydroxyglutarate (2-HG) production in several different IDH1 mutant AML cells within a 2-3 week time frame ex vivo. Because of the allosteric nature of the interaction, GSK321 is able to inhibit multiple mutant forms of IDH1, which is consistent with our cell biological observations. Furthermore, GSK321 retains excellent potency in cells, since it does not compete with the tightly bound cofactor. Synonyms: (7R)-1-[(4-fluorophenyl)methyl]-N-[3-[(1S)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrole-2-carbonyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-3-carboxamide; (7R)-1-[(4-fluorophenyl)methyl]-N-[3-[(1S)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrole-2-carbonyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-3-carboxamide; GSK321; GSK 321; GSK-321; BDBM195601. Grades: >98%. CAS No. 1816331-63-1. Molecular formula: C28H28FN5O3. Mole weight: 501.56.
GSK864
GSK864 is a cell penetrant, selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) mutant with IC50 values of 8.8, 15.2 and 16.6 nM for IDH1 mutants R132C, R132H, and R132G, respectively. Synonyms: (7S)-1-[(4-fluorophenyl)methyl]-3-N-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,6-dihydropyrazolo[4,3-c]pyridine-3,7-dicarboxamide; GSK 864; GSK-864. CAS No. 1816331-66-4. Molecular formula: C30H31FN6O4. Mole weight: 558.6.
IDH305
IDH305 is a potent, selective and brain penetrant inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 27, 28, and 6,140 nM for recombinant IDH1R132H, IDH1R132C, and wild-type IDH1, respectively). It suppresses mutant IDH1-dependent 2-HG production and cell proliferation, and exhibits antitumor activity in preclinical studies. Synonyms: (4R)-4-[(1S)-1-fluoroethyl]-3-[2-({(1S)-1-[4-methyl-2'-(trifluoromethyl)[3,4'-bipyridin]-6-yl]ethyl}amino)pyrimidin-4-yl]-1,3-oxazolidin-2-one. Grades: ≥98%. CAS No. 1628805-46-8. Molecular formula: C23H22F4N6O2. Mole weight: 490.45.
ML309
ML309 is a potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells. ML309 is capable of potent and selective inhibition of mutant IDH1 and effectively lowers cell-based production of 2-HG in a U87MG mutant glioblastoma cell line. Synonyms: ML-309; ML 309. Grades: 98%. CAS No. 1355446-05-7. Molecular formula: C29H29FN4O2. Mole weight: 484.56.
ML-309 hydrochloride
ML-309 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). It reduces 2-hydroxyglutarate production in U87 MG glioblastoma cells. Synonyms: ML 309 hydrochloride; ML309 hydrochloride; ML-309 HCl; 2-(N-[2-(benzimidazol-1-yl)acetyl]-3-fluoroanilino)-N-cyclopentyl-2-(2-methylphenyl)acetamide hydrochloride. Grades: ≥98%. CAS No. 1355327-02-4. Molecular formula: C29H29FN4O2·HCl. Mole weight: 521.
Mutant Isocitrate Dehydrogenase 1 R132H from Human, Recombinant
Mutations of the cytosolic IDH 1 are a common feature in primary human brain cancers. Arginine 132 (R132) of IDH is highly conserved among different isoforms of IDH and is most commonly mutated to Histidine. Mutation of IDH1 R132H leads to accumulation of R(-)-2-hydroxyglutarate (2HG), which correlates with an increased risk for malignant brain tumors. Full-length human idh1 (452 amino acids) with n-terminal hattag. arginine 132 is mutated to histidine. Group: Enzymes. Synonyms: Isocitrate dehydrogenase [NADP] cytoplasmic mutant, R132H; IDH 1 R132H. Purity: > 90% by SDS-PAGE. IDH. Mole weight: 50.9 kDa. Activity: >500 mU/mg. Storage: Lyophilized protein is stable for 1 year at -20°C. Once reconstituted aliquot and store at -20°C. Avoid repeated freeze/thaw cycles. Form: Lyophilized powder with additives. Source: E. coli. Species: Human. Isocitrate dehydrogenase [NADP] cytoplasmic mutant, R132H; IDH 1 R132H; Isocitrate dehydrogenase; Isocitrate Dehydrogenase (NADP+). Cat No: NATE-1649.
Olutasidenib
Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1) , with IC 50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively. Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: FT-2102. CAS No. 1887014-12-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-114226.
Olutasidenib
Olutasidenib is a mutant isocitrate dehydrogenase 1 (IDH1) inhibitor used to treat acute myeloid leukemia. Synonyms: FT-2102; FT2102. CAS No. 1887014-12-1. Molecular formula: C18H15ClN4O2. Mole weight: 354.8.
SCHEMBL14831541
SCHEMBL14831541, also called as Mutant IDH1 inhibitor, is an inhibitor of mutant IDH1 which is key enzymes found in cellular metabolism. Synonyms: Mutant IDH1 inhibitor; MDK-0084; MDK 0084; MDK0084; (4S) -3-[2-[[ (1S) -1-[4-[ (4-acetylpiperazin-1-yl) methyl]phenyl]ethyl]amino]pyrimidin-4-yl]-4-propan-2-yl-1, 3-oxazolidin-2-oneMutant IDH1 inhibitorSCHEMBL14831541BDBM146427; BDBM 146427; BDBM-146427CS-2102; CS 2102; CS2102HY-13972; HY 13972; HY13972US8957068, 556. CAS No. 1429180-08-4. Molecular formula: C25H34N6O3. Mole weight: 466.58.
TC-E 5008
TC-E 5008 is a selective and cancer-associated mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor (Ki = 120-190 nM), displaying >60-fold selectivity for mIDH1 (found in ~75% of gliomas) over wild type IDH1. TC-E 5008 also inhibits D-2-hydroxyglutaric acid in cells expressing mIDH1 (EC50 = 2.4 μM). Synonyms: 1-Hydroxy-4-methyl-6-(phenylmethyl)-2-(1H)pyridinone; 6-benzyl-1-hydroxy-4-methylpyridin-2-one. CAS No. 50405-58-8. Molecular formula: C13H13NO2. Mole weight: 215.25.
Vorasidenib
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC 50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. Vorasidenib can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AG-881. CAS No. 1644545-52-7. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-104042.
Vorasidenib
Vorasidenib is a potent and orally available pan-IDH (isocitrate dehydrogenase) mutant form inhibitor. It has the potential for the treatment of various cancers including glioma, acute myeloid leukemia (AML), cholangiocarcinoma and chondrosarcoma. Synonyms: AG-881; 6-(6-chloropyridin-2-yl)-2-N,4-N-bis[(2R)-1,1,1-trifluoropropan-2-yl]-1,3,5-triazine-2,4-diamine. CAS No. 1644545-52-7. Molecular formula: C14H13ClF6N6. Mole weight: 414.74.
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