Pamufetinib mesylate

Research use only, not for human use.

Pamufetinib mesylate (TAS-115 mesylate) is a potent vascular endothelial growth factor receptor (VEGFR) antagonist and hepatocyte growth factor receptor (c-Met) inhibitor used in the study of cancer and respiratory diseases.

Pamufetinib (TAS-115) mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.

Pamufetinib mesylate powerfully suppresses the VEGF-dependent proliferation of HUVECs (IC50=0.019 μM) as a VEGFR-targeted inhibitor and powerfully suppresses the proliferation of MET-amplified cancer cells (GI50=0.032-0.362 μM) as a MET-targeted inhibitor. Pamufetinib mesylate has much less toxicity in various normal cell lines when compared with other VEGFR-targeted kinase inhibitors. Crizotinib and Pamufetinib mesylate inhibit Met phosphorylation and reverse erlotinib resistance and VEGF production triggered by HGF in PC-9 and HCC827 cells.

Pamufetinib mesylate completely suppresses the progression of MET-inactivated tumor by blocking angiogenesis without toxicity when given every day for 6 weeks, even at a serum-saturating dose of Pamufetinib mesylate. Pamufetinib mesylate induces marked tumor shrinkage and prolonges survival in MET-amplified human cancer–bearing mice.

——

Angiogenesis

VEGFR

VEGFR | c-Met/HGFR

——

——

1688673-09-7

614.67

C28H27FN4O7S2

>98% (HPLC)

In Vitro:?DMSO : 75 mg/mL (122.02 mM; Ultrasonic )

O=C(NC)C1=CC=2C(=NC=CC2OC3=CC=C(C=C3F)NC(=S)NC(=O)CC=4C=CC=CC4)C=C1OC.O=S(=O)(O)C

——

(-20℃)

With Ice Pack

≥ 2 years