PHA-665752 | B2057

PHA-665752 is a potent, selective and ATP-competitive inhibitor of MET kinase (IC₅₀ values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKBα, p38α, MK2 and MK3). PHA665752 significantly reduces the tumor growth of NCI-H69, NCI-H441 and A549 in mouse xenografts by 99%, 75%, and 59%, respectively.

PHA-665752 is a potent, selective and ATP-competitive inhibitor of MET kinase (IC₅₀ values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKBα, p38α, MK2 and MK3). PHA665752 significantly reduces the tumor growth of NCI-H69, NCI-H441 and A549 in mouse xenografts by 99%, 75%, and 59%, respectively.

B2057 | PHA-665752 DataSheet

Alternate Name/Synonyms: 2R)-1-[[5-[(Z)-[5-[[(2,6-Dichlorophenyl)methyl]sulfonyl]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrol-3-yl]carbonyl]-2-(1-pyrrolidinylmethyl)pyrrolidine

Appearance: Yellow solid

Formulation: N/A

CAS Number: 477575-56-7

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₃₂H₃₄Cl₂N₄O₄S

Molecular Weight: 641.61

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (>50 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent, selective and ATP-competitive MET kinase inhibitor

MDL Number: MFCD07772270

PubChem CID: 10461815

SMILES: CC1=C(NC(=C1C(=O)N2CCCC2CN3CCCC3)C)C=C4C5=C(C=CC(=C5)S(=O)(=O)CC6=C(C=CC=C6Cl)Cl)NC4=O

InChi: InChI=1S/C32H34Cl2N4O4S/c1-19-29(35-20(2)30(19)32(40)38-14-6-7-21(38)17-37-12-3-4-13-37)16-24-23-15-22(10-11-28(23)36-31(24)39)43(41,42)18-25-26(33)8-5-9-27(25)34/h5,8-11,15-16,21,35H,3-4,6-7,12-14,17-18H2,1-2H3,(H,36,39)/b24-16-/t21-/m1/s1

InChi Key: OYONTEXKYJZFHA-SSHUPFPWSA-N