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Defactinib
- VS 6063 - PF 04554878
Axon 2574
CAS:
1073154-85-4
Purity:
98%
- Soluble in DMSO
- MF: C20H21F3N8O3S
- MW: 510.49
Description
Orally available second-generation inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase-2 (PYK2) with an acceptable safety profile in clinical trials (IC50 values 0.6 nM for each kinase, and >100-fold greater selectivity for FAK and PYK2 than for other, non-target kinases). Structurally closely related to PF 431396 (Axon 2107).
More Information
| Parent CAS No. | 1073154-85-4 |
|---|---|
| Chemical Name | N-methyl-4-(4-((3-(N-methylmethylsulfonamido)pyrazin-2-yl)methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)benzamide |
| SMILES | C1(C(F)(F)F)C=NC(NC2C=CC(C(NC)=O)=CC=2)=NC=1NCC1C(N(S(C)(=O)=O)C)=NC=CN=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C20H21F3N8O3S/c1-24-18(32)12-4-6-13(7-5-12)29-19-28-10-14(20(21,22)23)16(30-19)27-11-15-17(26-9-8-25-15)31(2)35(3,33)34/h4-10H,11H2,1-3H3,(H,24,32)(H2,27,28,29,30) |
| InChiKey | FWLMVFUGMHIOAA-UHFFFAOYSA-N |
| CID | 25117126 |
| Short Description | FAK/PYK2 inhibitor |
References
- YC Lee et al. Identification of Bone-Derived Factors Conferring De Novo Therapeutic Resistance in Metastatic Prostate Cancer. Cancer Res. 2015 Nov 15;75(22):4949-59.
- SF Jones et al. A phase I study of VS-6063, a second-generation focal adhesion kinase inhibitor, in patients with advanced solid tumors. Invest New Drugs. 2015 Oct;33(5):1100-7.
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