Volitinib dihydrochloride
- AZD6094 dihydrochloride - HMPL-504 dihydrochloride - Savolitinib dihydrochloride
- Parent CAS: 1313725-88-0
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C17H15N9.2HCl
- MW: 418.28
Description
Volitinib is an orally bioavailable ATP-competitive small molecule c-Met kinase inhibitor, binding to the enzyme potently with IC50 of 4 nM, and highly selective (>650 fold selectivity) over a panel of 265 kinases. Demonstrated selectivity for MET-driven disease, with MET amplified cell lines being most sensitive (IC50s of 1nM), and Displayed pote+DJ2869nt anti-tumor activity in cMET-dysregulated GC patient-derived tumor xenograft (PDX) models.
More Information
| Parent CAS No. | 1313725-88-0 |
|---|---|
| Chemical Name | (S)-1-(1-(imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine dihydrochloride |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1(C2=CN(C)N=C2)=NC2N([C@@H](C)C3C=CC4=NC=CN4C=3)N=NC=2N=C1.Cl.Cl |&1:10,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C17H15N9/c1-11(12-3-4-15-18-5-6-25(15)10-12)26-17-16(22-23-26)19-8-14(21-17)13-7-20-24(2)9-13/h3-11H,1-2H3/t11-/m0/s1 |
| InChiKey | XYDNMOZJKOGZLS-NSHDSACASA-N |
| CID | 68289010 |
| Short Description | c-Met kinase inhibitor |
References
- AG Schuller et al. The MET Inhibitor AZD6094 (Savolitinib, HMPL-504) Induces Regression in Papillary Renal Cell Carcinoma Patient-Derived Xenograft Models. Clin Cancer Res. 2015 Jun 15;21(12):2811-9.
- PR Gavine et al. Volitinib, a potent and highly selective c-Met inhibitor, effectively blocks c-Met signaling and growth in c-MET amplified gastric cancer patient-derived tumor xenograft models. Mol Oncol. 2015 Jan;9(1):323-33.
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