PHA-665752
PHA-665752 is a potent, ATP-competitive and specific c-Met receptor tyrosine kinase inhibitor with K(i) value of 4 nM and IC50 value of 9nM. PHA-665752 shows more than 50-fold selectivity for c-Met versus other serine-threonine and tyrosine kinases [1].
PHA-665752 has been demonstrated to inhibit hepatocyte growth factor (HGF) and c-Met-mediated cell proliferation, motility, invasion and morphology of pancreatic carcinoma cells BxPC-3, gastric carcinoma cells GTL-16 and lung cancer cells NCI-H441. Additionally, PHA-665752 inhibits the c-MET downstream mediators phosphorylation induced by HGF [1].
In vivo, PHA-665752 inhibits c-Met phosphorylation as well as tumor growth in both S114 and GTL-16 implanted xenograft athymic mice [1].
References:
[1] Christensen JG1, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R, Lipson KE, Ramphal J, Do S, Cui JJ,Cherrington JM, Mendel DB. 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. 2003 Nov 1;63(21):7345-55.
- 1. Anil Kumar Yadav, et al. "PHA-665752's Antigrowth and Proapoptotic Effects on HSC-3 Human Oral Cancer Cells." Int J Mol Sci. 2024 Mar 1;25(5):2871. PMID: 38474118
- 2. Hye-Min Jeon, Jeong-Yub Kim, et al. "Tissue factor is a critical regulator of radiation therapy-induced glioblastoma remodeling." Cancer Cell. 2023 Jul 11;S1535-6108(23)00217-9. PMID: 37451272
- 3. Xia Y, Xia YF, et al. "Madecassoside ameliorates bleomycin-induced pulmonary fibrosis in mice through promoting the generation of hepatocyte growth factor via PPAR-γ in colon. Br J Pharmacol." 2016 Apr;173(7):1219-35. PMID: 26750154
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 641.61 |
| Cas No. | 477575-56-7 |
| Formula | C32H34Cl2N4O4S |
| Solubility | insoluble in H2O; ≥3.1 mg/mL in EtOH with ultrasonic; ≥32.1 mg/mL in DMSO |
| Chemical 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 |
| SDF | Download SDF |
| 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | PHA-665752 is a potent, selective and ATP-competitive inhibitor of c-Met with IC50 of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs. | |||||
| Targets | c-Met | |||||
| IC50 | 9 nM | |||||
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
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Related Biological Data
