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PF-05139962 is a novel potent mTOR inhibitor with excellent mTOR biochemical inhibition, cellular potency, kinase selectivity and in vitro ADME properties. PF-05139962 has pS473 and pS6 cellular IC50 = 48 and 6 nM respectively. PF-05139962 has great selectivity against other receptors and kinases. No genotoxicity was observed on this compound and no more than 25% inhibiton was observed for major CYP enzymes (3A4, 1A2, 2C9, 2D6) at 3 uM. This compound has LE = 0.35 and LipE up to 6.8 which is in a very desirable range for a kinase inhibitor. Synonyms: PF 05139962; PF05139962. CAS No. 1393712-18-9. Molecular formula: C21H27N5O4S. Mole weight: 445.54.
PF 05175157
PF-05175157 is a selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 and isoform ACC2 dominant. IC50 values are 27 nM and 33 nM, respectively. It was originated by Pfizer. ACC inihibitors can inhibit de novo lipogenesis and increase β-oxidation of long-chain fatty acids. In Feb 2015, Phase-II for Type-2 diabetes mellitus in USA was discontinued. Uses: Type 2 diabetes mellitus. Synonyms: PF-05175157; PF05175157; 1,4-Dihydro-1'-[(2-methyl-1H-benzimidazol-6-yl)carbonyl]-1-(1-methylethyl)-spiro[5H-indazole-5,4'-piperidin]-7(6H)-one. Grades: 98%. CAS No. 1301214-47-0. Molecular formula: C23H27N5O2. Mole weight: 405.50.
PF 05180999 is a potent and selective PDE2A inhibitor (IC50 = 1 nM), with 2000-fold selectivity for PDE2A over PDE10A. PF 05180999 was evaluated for schizophrenia and migraine, but no further development has been reported since 2014. Synonyms: 4-(1-Azetidinyl)-7-methyl-5-[1-methyl-5-[5-(trifluoromethyl)-2-pyridinyl]-1H-pyrazol-4-yl]-imidazo[5,1-f][1,2,4]triazine; PF05180999; PF-05180999; PF 5180999; PF5180999; PF-5180999; PF 5180999; PF999; PF-999; PF 999. Grades: ≥98% by HPLC. CAS No. 1394033-54-5. Molecular formula: C19H17F3N8. Mole weight: 414.39.
Potent and selective dual inhibitor of PI 3-kinase/mTOR (IC50 values are 0.4, 1.6 and 5.4nm for PI 3-Kalpha, mTOR and PI 3-Kgamma respectively). Exhibits selectivity over 234 other protein kinases (IC50 >10um). Potently inhibits tumor cell growth in 37 different tumor cell lines (IC50 < 100nm). Also exhibits antitumor activity in MDA-361, HCT-116, H1975 and U87MG xenograft models. Group: Biochemicals. Grades: Highly Purified. CAS No. 1197160-78-3. Pack Sizes: 10mg. US Biological Life Sciences.
PF-05231023 is a long-acting FGF21 mimic. PF-05231023 can reduce the weight of non-human primates and patients with type 2 diabetes and improve blood lipid status. It is a PEG-based PROTAC linker that can be used to synthesize PROTAC. Synonyms: Mal-Amido-PEG2-C2-Amido-Ph-C2-CO-AZD; 2, 5-Dihydro-2, 5-Dioxo-N- (2- (2- (3-Oxo-3- ( (4- (3-Oxo-3- (2-Oxo-1-Azetidinyl) Propyl) Phenyl) Amino) Propoxy) Ethoxy) Ethyl) -1H-Pyrrole-1-Propanamide; 2, 5-Dihydro-2, 5-Dioxo-N- [2- [2- [3-Oxo-3- [ [4- [3-Oxo-3- (2-Oxo-1-Azetidinyl) Propyl] Phenyl] Amino] Propoxy] Ethoxy] Ethyl] -1H-Pyrrole-1-Propanamide. Grades: ≥98% by HPLC. CAS No. 1037589-69-7. Molecular formula: C26H32N4O8. Mole weight: 528.6.
PF-05241328, a purely acidic molecule, is a selective inhibitor of human Nav1. 7 voltage-dependent sodium channels (IC50 = 31nM) for the treatment of pain. But PF-05241328 is studied to have poor solubility and likely solubility limited absorption. Synonyms: PF-05241328; PF 05241328; PF05241328; PF-5241328; PF 5241328; PF5241328. 1-(5-Chloro-6-(2-methylpropoxy)-3-pyridinyl)-3-methyl-N-(methylsulfonyl)-1H-indazole-5-carboxamide; 1H-Indazole-5-carboxamide, 1-(5-chloro-6-(2-methylpropoxy)-3-pyridinyl)-3-methyl-N-(methylsulfonyl)-. CAS No. 1387633-03-5. Molecular formula: C19H21ClN4O4S. Mole weight: 436.9179.
PF-05274857 Hydrochloride
PF-05274857 Hydrochloride. Group: Biochemicals. Alternative Names: 1-(4-(5'-Chloro-3,5-dimethyl-[2,4'-bipyridin]-2'-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one Monohydrochloride. Grades: Highly Purified. Pack Sizes: 2.5mg. Molecular Formula: C20H26Cl2N4O3S, Molecular Weight: 473.42. US Biological Life Sciences.
Worldwide
PF-05297909
PF-05297909, is a BACE inhibitor developed by Pfizer. Phase 1. Synonyms: PF-05297909; PF-5297909.
PF 06260933 is a highly selective, orally active and small-molecule inhibitor of MAP4K4 (Mitogen-activated protein kinase kinase kinase kinase 4) (IC50 = 140 nM). It also inhibits MINK and TNIK (IC50= 8 and 13 nM, respectively). PF-06260933 dihydrochloride has been shown to improves fasting hyperglycemia in mice. Synonyms: 5-(4-Chlorophenyl)-[3,3'-bipyridine]-6,6'-diamine dihydrochloride; PF-06260933 dihydrochloride; PF06260933 dihydrochloride; PF 06260933 dihydrochloride. Grades: ≥98% by HPLC. CAS No. 1883548-86-4. Molecular formula: C16H13ClN4.2HCl. Mole weight: 369.68.
PF 06273340 is a potent and selective, orally bioavailable pan-Trk kinase inhibitor with IC50 of 6, 2, and 1 nM for Trk A, B and C, respectively. PF 06273340 is selective for Trk over a panel of ion channels, receptors and other enzymes. It shows efficacy in a rodent model of inflammatory pain. Synonyms: N-[5-[[2-Amino-7-(2-hydroxy-1,1-dimethylethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]carbonyl]-3-pyridinyl]-5-chloro-2-pyridineacetamide; PF-06273340; PF 06273340; PF06273340; PF-6273340; PF 6273340; PF6273340. Grades: ≥98% by HPLC. CAS No. 1402438-74-7. Molecular formula: C23H22ClN7O3. Mole weight: 479.93.
PF-06282999 is a selective myeloperoxidase Inhibitor originate by Pfizer. It showed good oral pharmacokinetics in preclinical species and robust irreversible inhibition of plasma MPO activity. In Mar 2015, Pfizer terminated phase I trial for the treatment of Acute coronary syndromes in Healthy volunteers in USA. Uses: Acute coronary syndromes. Synonyms: PF-06282999; PF06282999; PF06282999. 2-(6-(5-chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide. Grades: 98%. CAS No. 1435467-37-0. Molecular formula: C13H12ClN3O3S. Mole weight: 325.77.
PF-06372222 is a small molecule negative allosteric modulator (NAM) of glucagon receptor (GCGR), which helps treat type 2 diabetes. It is also an antagonist of the glucagon-like peptide-1 receptor GLP-1R, which can inhibit glucagon secretion and glucose-dependent insulin secretion. Synonyms: N-{4-[(R)-(3,3-Dimethylcyclobutyl)({6-[4-(Trifluoromethyl)-1h-Imidazol-1-Yl]Pyridin-3-Yl}Amino)Methyl]Benzene-1-Carbonyl}-Beta-Alanine. Grades: ≥98% by HPLC. CAS No. 1407592-99-7. Molecular formula: C26H28F3N5O3. Mole weight: 515.5.
PF-06372865
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABA A positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABA A receptors containing α1/α2/α3/α5 subunits ( K i s of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1614245-70-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-120874.
PF 06409577
PF 06409577 is a potent and selective allosteric activator of AMPK (EC50 values are 7 and >40000 nM for AMPKα1β1γ1 and AMPKα1β2γ1, respectively) for the potential treatment of diabetic nephropathy. PF-06409577 showed efficacy in a preclinical model of diabetic nephropathy. Synonyms: PF-06409577; PF06409577; PF-6409577; PF6409577; PF 6409577. Grades: ≥98% by HPLC. CAS No. 1467057-23-3. Molecular formula: C19H16ClNO3. Mole weight: 341.79.
PF 06424439 is a potent, selective and orally bioavailable Diacylglycerol Acyltransferase 2 ( DGAT2) inhibitor with DGAT2 IC50 ± SEM (nM) (human/rat/dog) 14 ± 1/38 ± 4/16 ± 1, which exhibits no significant activity at MGAT1-3 or DGAT1. It reduces triglyderide synthesis in human hepatocytes in vitro, and reduces plasma triglyceride and cholesterol levels in a rat dyslipidemia model. Synonyms: [(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinylmethanone methanesulfonate; PF-06424439; PF06424439; PF 06424439; PF-6424439; PF-6424439; PF 6424439. Grades: ≥98% by HPLC. CAS No. 1469284-79-4. Molecular formula: C22H26ClN7O.CH4O3S. Mole weight: 536.05.
PF-06424439, a imidazo-pyridin derivative, has been found to be a selective DGAT2 inhibitor that could be probably effective against dyslipidemic rodent in animal models. Synonyms: PF-06424439; PF06424439; PF 06424439; PF-6424439; PF-6424439; PF 6424439; (R)-(1-(2-(1-(4-chloro-1H-pyrazol-1-yl)cyclopropyl)-3H-imidazo[4,5-b]pyridin-5-yl)piperidin-3-yl)(pyrrolidin-1-yl)methanone. Grades: 98%. CAS No. 1469284-78-3. Molecular formula: C22H26ClN7O. Mole weight: 439.94.
PF-06442609 is a potent, metabolic stable γ-secretase modulators. It displayed a favorable rodent pharmacokinetic profile, and robust reductions of brain Aβ42 and Aβ40 were observed in a guinea pig time-course experiment. F-06442609 may be used for the treatment of Alzheimer's disease in the future. Uses: Alzheimer's disease. Synonyms: PF-06442609; PF 06442609; PF06442609; PF-6442609; PF 6442609; PF6442609. 2-((S)-1-(4-fluoro-2-((R)-1,1,1-trifluoropropan-2-yl)phenoxy)propan-2-yl)-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione. Grades: 98%. CAS No. 1402002-76-9. Molecular formula: C24H24F4N4O3. Mole weight: 492.47.
PF06447475 is a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. Leucine rich repeat kinase 2 (LRRK2) has been genetically linked to Parkinson's disease (PD) by genome-wide association studies (GWAS). The most common LRRK2 mutation, G2019S, which is relatively rare in the total population, gives rise to increased kinase activity. As such, LRRK2 kinase inhibitors are potentially useful in the treatment of PD. Synonyms: PF06447475; PF-06447475; PF 06447475; PF6447475; PF-6447475; PF 6447475. Grades: >98%. CAS No. 1527473-33-1. Molecular formula: C17H15N5O. Mole weight: 305.33.
PF-06459988 is a third-generation, irreversible epidermal growth factor receptor (EGFR) inhibitor. It can bind to and inhibit mutant forms of EGFR, including the secondary acquired resistance mutation T790M.PF-06459988 may have therapeutic benefits in tumors with T790M-mediated drug resistance. Preclinical trials in Non-small cell lung cancer in USA is on-going. Uses: Non-small cell lung cancer. Synonyms: PF-06459988; PF06459988; PF 06459988; PF-6459988; PF 6459988; PF6459988; 1-((3R,4R)-3-(((5-chloro-2-((1-methyl-1H-pyrazol-4-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)methyl)-4-methoxypyrrolidin-1-yl)prop-2-en-1-one. Grades: 98%. CAS No. 1428774-45-1. Molecular formula: C19H22ClN7O3. Mole weight: 431.88.
PF-06471553, isoindoline-5-sulfonamide, selectively inhibits MGAT3 with high in vitro potency and cell efficacy which displayed suitable PK properties in mouse and in vivo MGAT3 inhibition in a transgenic mouse model. Synonyms: PF-06471553; PF 06471553; PF06471553; PF-6471553; PF 6471553; PF6471553. N-(2-cyclobutyl-2H-1,2,3-triazol-4-yl)-2-(2-(3-methoxyphenyl)acetyl)isoindoline-5-sulfonamide. Grades: >98%. CAS No. 1808094-07-6. Molecular formula: C23H25N5O4S. Mole weight: 467.54.
PF 06551600 malonate
PF 06551600 is a potent and selective JAK3 inhibitor with IC50 value of 33.1 μM, exhibiting >1,000-fold selectivity over JAK1 and JAK2. It inhibits phosphorylation of STAT5, induced by IL-2, IL-4, IL-7 and IL-15. It also inhibits Th1 and Th17 T-cell differentiation and function in vitro. Synonyms: 1-[(2S,5R)-2-Methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one malate. Grades: ≥98% by HPLC. CAS No. 2140301-97-7. Molecular formula: C15H19N5O·C3H4O4. Mole weight: 389.41.
PF-06648671
PF-06648671 is a novel, brain-penetrable, and orally active γ-secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimers disease [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1587727-31-8. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-120789.
PF-06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), which is an omnipresently expressed serine/threonine kinase involved in the regulation of innate immunity. PF-06650833 is useful for the treatment of autoimmune and inflammatory diseases associated with lnterleukin-1 Receptor Associated Kinase (IRAK) and more particularly modulates the function of IRAK. It is undergoing testing in a Phase II clinical study. Synonyms: zimlovisertib; PF 06650833; PF06650833. CAS No. 1817626-54-2. Molecular formula: C18H20FN3O4. Mole weight: 361.373.
PF-06651600 is a selective JAK3 inhibitor with IC50 value of 0.346 nM. It was shown to inhibit Th1 and Th17 cell differentiation and function in vitro. Synonyms: Ritlecitinib; PF 06651600; PF06651600; 2-Propen-1-one, 1-[(2S,5R)-2-methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-. Grades: >98%. CAS No. 1792180-81-4. Molecular formula: C15H19N5O. Mole weight: 285.351.
PF-06700841 is a potent and selective inhibitor of TYK2 and JAK1. It has the potential to treat plaque psoriasis and lupus erythematosus. Synonyms: Brepocitinib tosylate; [(1S)-2,2-difluorocyclopropyl]-[(1R,5S)-3-[2-[(1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-3,8-diazabicyclo[3.2.1]octan-8-yl]methanone tosylate. Grades: ≥98%. CAS No. 2140301-96-6. Molecular formula: C18H21F2N7O·C7H8O3S. Mole weight: 561.61.