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Product name : PND-1186
Item : CR2018
CAS : 1061353-68-1
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Details:

Biological Activity of PND-1186

PND-1186 is a potent FAK inhibitor with IC50 of 1.5 nM.
IC50 Value: 1.5 nM [1]
Target: FAK
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 [1].
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 [1]. 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 [2].
Clinical trial: Phase I, Dose-Escalation Study of VS-4718 in Subjects With Metastatic Non-Hematological Malignancies. Phase 1
 

Chemical Information

M.Wt 501.5 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C25H26F3N5O3
CAS No 1061353-68-1
Solvent & Solubility

10 mM in DMSO

Preparing Stock Solutions

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

Clinical Information of PND-1186

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

References on PND-1186

 

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