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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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P125191-5mg | 5mg | In stock | $73.90 | |
P125191-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $112.90 | |
P125191-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $360.90 |
Potent, selective, ATP-competitive c-Met inhibitor
Synonyms | PHA-665752 hydrate | (3Z)-5-{[(2,6-dichlorophenyl)methane]sulfonyl}-3-[(3,5-dimethyl-4-{[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]carbonyl}-1H-pyrrol-2-yl)methylidene]-2,3-dihydro-1H-indol-2-one | 2H-Indol-2-one, 5-(((2,6-dichlorophenyl)methyl)sulfon |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | PHA-665752 is 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, PKB&al |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of MET proto-oncogene; receptor tyrosine kinase |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | PHA-665752 hydrate has been used as a c-Met inhibitor:
to study its effects on oxidative stress in human mammary epithelial MCF10A cells with extra centrosomes
to study its effects on the clonogenicity of T-cell specific transcription factor/ lymphoid enhancer-binding factor-1 (TCF/LEF-1) responsive promoter to drive expression of green fluorescent protein (TOP-GFP) cancer stem cell (CSC) cultures
to study its inhibitory effects on melanoma cell lines |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | (3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one |
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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 |
Canonical 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 |
Isomeric SMILES | CC1=C(NC(=C1C(=O)N2CCC[C@@H]2CN3CCCC3)C)/C=C\4/C5=C(C=CC(=C5)S(=O)(=O)CC6=C(C=CC=C6Cl)Cl)NC4=O |
PubChem CID | 10461815 |
Molecular Weight | 641.61 |
CAS Registry No. | 477575-56-7 |
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DiscoveRx TREEspot | PHA-665752| |
PubChem CID | 10461815 |
ChEMBL Ligand | CHEMBL450786 |
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Solubility | DMSO 128 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
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1. Christensen JG, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R et al.. (2003) A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo.. Cancer Res, 63 (21): (7345-55). [PMID:14612533] [10.1021/op500134e] |