PHA 665752 (CAS 477575-56-7)
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PHA 665752 is a cell-permeable pyrrolo-indolinone compound that acts as an ATP-competitive and highly potent inhibitor of Met tyrosine kinase activity (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) with good selectivity in both cell-free kinase assays (7.5-, 22-, 155-, and ≥333-fold over Ron, Flk1, c-abl, and a panel of 12 other commonly studied kinases, respectively) and in receptor autophosphorylation in cells (20- and 60-fold over Ron and Flk1, respectively). PHA 665752 is shown to suppress Met-mediated cellular functions in vitro and inhibit tumorigenicity in various murine tumor models in vivo. PHA 665752 is an antitumor agent and inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.
PHA 665752 (CAS 477575-56-7) References
- A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. | Christensen, JG., et al. 2003. Cancer Res. 63: 7345-55. PMID: 14612533
- A selective c-met inhibitor blocks an autocrine hepatocyte growth factor growth loop in ANBL-6 cells and prevents migration and adhesion of myeloma cells. | Hov, H., et al. 2004. Clin Cancer Res. 10: 6686-94. PMID: 15475459
- Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. | Smolen, GA., et al. 2006. Proc Natl Acad Sci U S A. 103: 2316-21. PMID: 16461907
- A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. | Puri, N., et al. 2007. Cancer Res. 67: 3529-34. PMID: 17440059
- A selective small molecule inhibitor of c-Met, PHA-665752, reverses lung premalignancy induced by mutant K-ras. | Yang, Y., et al. 2008. Mol Cancer Ther. 7: 952-60. PMID: 18413809
- Effects of PHA-665752 and Cetuximab Combination Treatment on In Vitro and Murine Xenograft Growth of Human Colorectal Cancer Cells with KRAS or BRAF Mutations. | Jia, YT., et al. 2018. Curr Cancer Drug Targets. 18: 278-286. PMID: 28359236
- Effects of PHA-665752 and vemurafenib combination treatment on in vitro and murine xenograft growth of human colorectal cancer cells with BRAFV600E mutations. | Zhi, J., et al. 2018. Oncol Lett. 15: 3904-3910. PMID: 29456739
- Hepatocyte Growth Factor (HGF) Promotes Peripheral Nerve Regeneration by Activating Repair Schwann Cells. | Ko, KR., et al. 2018. Sci Rep. 8: 8316. PMID: 29844434
- A selective small-molecule inhibitor of c-Met suppresses keloid fibroblast growth in vitro and in a mouse model. | Choi, MH., et al. 2021. Sci Rep. 11: 5468. PMID: 33750878
- A c-Met Inhibitor Suppresses Osteosarcoma Progression via the ERK1/2 Pathway in Human Osteosarcoma Cells. | Chen, W., et al. 2021. Onco Targets Ther. 14: 4791-4804. PMID: 34531665
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PHA 665752, 2 mg | sc-203186 | 2 mg | $140.00 | |||
PHA 665752, 10 mg | sc-203186A | 10 mg | $275.00 | |||
PHA 665752, 50 mg | sc-203186B | 50 mg | $700.00 | |||
PHA 665752, 200 mg | sc-203186C | 200 mg | $1480.00 |