Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(SR-2516; PND 1186; PND1186; SR 2516; SR2516; VS-4718; VS 4718; VS4718)
PND-1186 Chemical Structure
|Product name: PND-1186|
|Cat. No.: HY-13917|
PND-1186 is a potent FAK inhibitor with IC50 of 1.5 nM.
IC50 Value: 1.5 nM 
in vitro: PND-1186 has an IC50 of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397. PND-1186 did not alter c Src or p130Cas tyrosine phosphorylation in adherent cells, yet functioned to restrain cell movement. Notably, 1.0 ?M PND-1186 (>5-fold above IC50) had limited effects on cell proliferation. However, under non-adherent conditions as spheroids and as colonies in soft agar, 0.1 ?M PND-1186 blocked FAK and p130Cas tyrosine phosphorylation, promoted caspase-3 activation, and triggered cell apoptosis .
in vivo: Addition of PND-1186 to the drinking water of mice was well tolerated and inhibited ascites- and peritoneal membrane-associated ovarian carcinoma tumor growth associated with the inhibition of FAK Tyr-397 phosphorylation . PND-1186 (100 mg/kg intraperitoneal, i.p.) showed promising pharmacokinetics (PK) and inhibited tumor FAK Tyr-397 phosphorylation for 12 hours. Oral administration of 150 mg/kg PND-1186 gave a more sustained PK profile verses i.p., and when given twice daily, PND-1186 significantly inhibited sygeneic murine 4T1 orthotopic breast carcinoma tumor growth and spontaneous metastasis to lungs .
Clinical trial: Phase I, Dose-Escalation Study of VS-4718 in Subjects With Metastatic Non-Hematological Malignancies. Phase 1
|M.Wt||501.5||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 34 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||1.9940 mL||9.9701 mL||19.9402 mL|
|5 mM||0.3988 mL||1.9940 mL||3.9880 mL|
|10 mM||0.1994 mL||0.9970 mL||1.9940 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|PND-1186||Verastem Inc||Metastasis||30-JUN-13||31-DEC-14||Phase 1||25-NOV-13|
NVP-TAE226 is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2(IC50=3.5 nM); 10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.
PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively), PF-431396 has a Kd value of 445 nM for BRD4.
PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for inhibiton of purified recombinant catalytic fragment of FAK; inhibits FAK phosphorylation on Tyr(397) with an IC(50) of 30-100 nM.
Y15 is a novel small molecule FAK phosphorylation inhibitor; specifically block phosphorylation of Y397-FAK and total phosphorylation of FAK.