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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|
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