AST 487

AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.

Product Specifications

CAS Number

[630124-46-8]

Product Name Alternative

NVP-AST 487

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Bcr-Abl; c-Kit; FLT3; RET; VEGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/AST-487.html

Purity

98.90

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C(NC1=CC=C(OC2=NC=NC(NC)=C2)C=C1)NC3=CC=C(CN4CCN(CC)CC4)C(C(F)(F)F)=C3

Molecular Formula

C26H30F3N7O2

Molecular Weight

529.56

Precautions

H302, H315, H319, H335

References & Citations

[1]Akeno-Stuart N, et al. The RET Kinase Inhibitor NVP-AST487 Blocks Growth and Calcitonin Gene Expression through Distinct Mechanisms in Medullary Thyroid Cancer Cells. Cancer Res. 2007 Jul 15;67 (14) :6956-64.|[2]Weisberg E, et al. Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cells. Blood. 2008 Dec 15;112 (13) :5161-70.