Ningetinib Tosylate

Research use only, not for human use.

Ningetinib Tosylate is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively.

Ningetinib Tosylate is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively.

Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. In cell-based functional assays, Ningetinib Tosylate (CT053PTSA) inhibits HGF and VEGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC50 values of 8.6 and 6.3 nM, respectively.

When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib Tosylate (CT053PTSA) potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours in tumor tissues. In orthotopic U87MG human glioblastoma xenograft model, Ningetinib Tosylate prolongs the median survival time (MST) and yields significant increase in life-span value (ILS=32%, p=0.003) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group.

——

Tyrosine Kinase

TAM Receptor

AXL|c-Met|VEGFR2

——

——

1394820-77-9

728.79

C38H37FN4O8S

>98% (HPLC)

DMSO:8 mg/mL (10.98 mM; Need ultrasonic and warming)

O=C(C1=C(C)N(C)N(C2=CC=CC=C2)C1=O)NC3=CC=C(OC4=CC=NC5=CC(OCC(C)(O)C)=CC=C45)C(F)=C3.CC6=CC=C(S(=O)(O)=O)C=C6

——

(-20℃)

With Ice Pack

≥ 2 years