Bulk Inquiry
PND 1186
- SR 2516 - VS 4718
- Soluble in DMSO
- MF: C25H26F3N5O3
- MW: 501.5
Description
Orally active dual FAK/PYK2 inhibitor (IC50 value 1.5 nM and ~100 nM in vitro and in vivo, respectively) that blocks FAK and p130Cas (130 kDa Crk-associated substrate) tyrosine phosphorylation, promotes caspase-3 activation, and selectively triggered cell apoptosis in tumor cells in 3D environments. PND1186 inhibitory effects differ from Dasatinib (Axon 1392; as it does not affect c-Src activity), and prevents spontaneous breast to lung metastasis in pre-clinical models. PND-1186 inhibits cell growth in multiple myeloma (MM) cells both in vitro and in vivo by inhibition of PYK2 (IC50 and EC50 values 85 nM and 20 nM, respectively).
More Information
| Parent CAS No. | 1061353-68-1 |
|---|---|
| Chemical Name | 2-(2-(2-methoxy-4-morpholinophenylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-N-methylbenzamide |
| SMILES | C(NC)(=O)C1=CC=CC=C1NC1C(C(F)(F)F)=CN=C(NC2=CC=C(N3CCOCC3)C=C2OC)C=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C25H26F3N5O3/c1-29-24(34)17-5-3-4-6-19(17)31-21-14-23(30-15-18(21)25(26,27)28)32-20-8-7-16(13-22(20)35-2)33-9-11-36-12-10-33/h3-8,13-15H,9-12H2,1-2H3,(H,29,34)(H2,30,31,32) |
| InChiKey | IGUBBWJDMLCRIK-UHFFFAOYSA-N |
| CID | 25073775 |
| Short Description | FAK/PYK2 inhibitor |
References
- I. Tanjoni et al. PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Cancer Biol Ther. 2010 May 15;9(10):764-77.
- C. Walsh et al. Oral delivery of PND-1186 FAK inhibitor decreases tumor growth and spontaneous breast to lung metastasis in pre-clinical models. Cancer Biol Ther. 2010 May 15;9(10):778-90.
- Y. Zhang et al. Pyk2 promotes tumor progression in multiple myeloma. Blood. 2014 Oct 23;124(17):2675-86.
Other Categories
Are you sure you would like to remove this item from the shopping cart?
This item is a part of the approved quote. Removing it will remove all quote items from the cart.