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Defactinib hydrochloride

Chemical Structure : Defactinib hydrochloride

CAS No.: 1073160-26-5

Defactinib hydrochloride (VS-6063;VS6063;PF04554878;PF-04554878)

Catalog No.: PC-42952Not For Human Use, Lab Use Only.

Defactinib (VS-6063,PF-04554878) is a potent, selective and orally active FAK inhibitor, inhibits pFAK (Tyr397) in a dose-dependent manner in cancer cell lines.

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10 mg $98 In stock
25 mg $158 In stock
50 mg $248 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Defactinib (VS-6063,PF-04554878) hydrochloride is a potent, selective and orally active FAK inhibitor, inhibits pFAK (Tyr397) in a dose-dependent manner in cancer cell lines.
Defactinib shows no statistically significant changes in FAK phosphorylation at the other residues(Tyr 576/577, Tyr 925, or Tyr 861), also inhibits Pyk2 Tyr402 phosphorylation in HeyA8 cells.
Defactinib markedly decreases proliferation and increases apoptosis combined with paclitaxel, reduces levels of AKT and YB-1 in taxane-resistant cell lines.
Defactinib significantly reduces tumor growth, synergized with the mTOR inhibitor everolimus in xenograft models of pancreatic tumor.

Physicochemical Properties

M.Wt 546.9537
Formula C20H22ClF3N8O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzamide, N-methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-, hydrochloride (1:1)

References

1. Kang Y, et al. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95.

2. Shimizu T, et al. Cancer Chemother Pharmacol. 2016 May;77(5):997-1003.

3. Jones SF, et al. Invest New Drugs. 2015 Oct;33(5):1100-7.

4. François RA, et al. J Natl Cancer Inst. 2015 May 12;107(8). pii: djv123.

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