AST487

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WARNING: This product is for research use only, not for human or veterinary use.

Description:AST487, also known as NVP-AST487, is a RET kinase inhibitor/FLT3 inhibitor. The RET kinase has emerged as a promising target for the therapy of medullary thyroid cancers (MTC) and of a subset of papillary thyroid cancers. NVP- AST487 has an IC(50) of 0.88 mumol/L on RET kinase, inhibits RET autophosphorylation and activation of downstream effectors, and potently inhibited the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations. NVP- AST487 induced a dose-dependent growth inhibition of xenografts of NIH3T3 cells expressing oncogenic RET, and of the MTC cell line TT in nude mice. NVP- AST487 inhibited calcitonin gene expression in vitro in TT cells, in part, through decreased gene transcription.

Price and Availability

AST487, purity > 98%, is in stock. The same day shipping after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406211Name: AST487CAS#: 630124-46-8Chemical Formula: C26H30F3N7O2Exact Mass: 529.24131Molecular Weight: 529.56Elemental Analysis: C, 58.97; H, 5.71; F, 10.76; N, 18.51; O, 6.04

Synonym:NVP AST487; NVP AST-487; NVP AST 487; NVP-AST487; NVP-AST-487; NVP-AST 487; AST 487; AST487; AST-487.

IUPAC/Chemical Name:1-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(4-((6-(methylamino)pyrimidin-4-yl)oxy)phenyl)urea

InChi Key:ODPGGGTTYSGTGO-UHFFFAOYSA-N

InChi Code:InChI=1S/C26H30F3N7O2/c1-3-35-10-12-36(13-11-35)16-18-4-5-20(14-22(18)26(27,28)29)34-25(37)33-19-6-8-21(9-7-19)38-24-15-23(30-2)31-17-32-24/h4-9,14-15,17H,3,10-13,16H2,1-2H3,(H,30,31,32)(H2,33,34,37)

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

Technical Data

Additional Information

References

1: Weisberg E, Roesel J, Furet P, Bold G, Imbach P,Flörsheimer A, Caravatti G, Jiang J, Manley P, Ray A, Griffin JD.Antileukemic Effects of Novel First- and Second-Generation FLT3Inhibitors: Structure-Affinity Comparison. Genes Cancer. 2010Oct;1(10):1021-32. doi: 10.1177/1947601910396505. PubMed PMID: 21779428;PubMed Central PMCID: PMC3092267.

2: Weisberg E, Roesel J, Bold G, Furet P, Jiang J, Cools J, Wright RD,Nelson E, Barrett R, Ray A, Moreno D, Hall-Meyers E, Stone R, GalinskyI, Fox E, Gilliland G, Daley JF, Lazo-Kallanian S, Kung AL, Griffin JD.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. doi: 10.1182/blood-2008-02-138065. Epub2008 Sep 26. PubMed PMID: 18820131; PubMed Central PMCID: PMC2597611.

3: Akeno-Stuart N, Croyle M, Knauf JA, Malaguarnera R, Vitagliano D,Santoro M, Stephan C, Grosios K, Wartmann M, Cozens R, Caravatti G,Fabbro D, Lane HA, Fagin JA. The RET kinase inhibitor NVP-AST487 blocksgrowth and calcitonin gene expression through distinct mechanisms inmedullary thyroid cancer cells. Cancer Res. 2007 Jul 15;67(14):6956-64.PubMed PMID: 17638907.