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In mice bearing 4T1 tumors, PND-1186 (100 mg/kg s.c.) inhibits 4T1 subcutaneous tumor growth by induction of apoptosis. In mice bearing ID8 tumors, PND-1186 (0.5 mg/mL for p.o.) also causes ovarian carcinoma tumor growth inhibition.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.
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Source | Cell Death Differ (2017). Figure 8. PND-1186 |
| Method | cell proliferation assay | |
| Cell Lines | HCC cells | |
| Concentrations | 1 μM | |
| Incubation Time | 48 h | |
| Results | As expected, 1 μM PND-1186 significantly downregulated EZH2 mRNA and upregulated NOTCH2 expression |
| Molecular Weight | 501.5 |
| Formula | C25H26F3N5O3 |
| CAS Number | 1061353-68-1 |
| Solubility (25°C) | DMSO 24 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related FAK Products |
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| NVP-TAE226
Nvp-tae 226 (TAE226) is a potent atP-competitive dual FAK and IGF-1R inhibitor with IC50 of 5.5 nM and 140 nM, respectively. Nvp-tae 226 (TAE226) also effectively inhibited Pyk2, insulin receptor (InsR), with IC50 of 3.5 nM and 40 nM. |
| PF-562271
PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively. |
| PF-573228
PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. |
| PF-00562271
PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. |
| Defactinib
Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor, with potential antiangiogenic and antineoplastic activities. |
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