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Merck
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SML2363

Sigma-Aldrich

AST487

≥98% (HPLC)

别名:

1-(4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(4-(6-(methylamino)pyrimidin-4-yloxy)phenyl)urea, AST 487, AST-487, N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N′-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea, NVP-AST 487, NVP-AST-487, NVP-AST487

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About This Item

经验公式（希尔记法）:
C26H30F3N7O2
CAS号:
630124-46-8
分子量:
529.56
MDL编号:
MFCD11983171
UNSPSC代码:
12352200
价格与库存信息目前不能提供

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

−20°C

SMILES字符串

CCN1CCN(CC2=C(C(F)(F)F)C=C(NC(NC3=CC=C(OC4=NC=NC(NC)=C4)C=C3)=O)C=C2)CC1

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)

InChI key

ODPGGGTTYSGTGO-UHFFFAOYSA-N

生化/生理作用

AST487 is an orally available type II tyrosine kinase inhibitor (TKI) that exhibits potent antiproliferation activity against FLT3, RET, PDGFR1, but not BRAF, oncogenic fusions/mutations-driven growth (IC50 = 1.8 nM/FLT3-ITD BaF3, 5.1 nM/FLT3 D835I BaF3, 9-27 nM/TEL-PDGFR1 & PTC3-RET BaF3, <1 nM/FLT3-ITD-expressing MV4-11 &amp; MOLM-13) via binding/stablizing target kinases in the inactive “DFG-out” conformation. AST487 effectively suppresses RET- (NIH3T3-RETC634W & human medullary thyroid cancer (MTC) TT cells) and FLT3-ITD-driven (MV4-11) tumor growth in mice in vivo (20-50 mg/kg/day p.o.).
AST487 is a N,N′-diphenyl urea, which inhibits growth and calcitonin gene expression in medullary thyroid cancer cells.[1]
Orally active, type II tyrosine kinase inhibitor against FLT3, RET, and PDGFR1 oncogenic fusions/mutations-driven growth in vitro and in vivo.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000059028
0000059029
0000048692

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Ellen Weisberg et al.
Genes & cancer, 1(10), 1021-1032 (2011-07-23)
Constitutively activated mutant FLT3 has emerged as a promising target for therapy for the subpopulation of acute myeloid leukemia (AML) patients who harbor it. The small molecule inhibitor, PKC412, targets mutant FLT3 and is currently in late-stage clinical trials. However
Yu-Lin Hsieh et al.
Experimental neurology, 300, 87-99 (2017-11-07)
Neurotrophic factors and their corresponding receptors play key roles in the maintenance of different phenotypic dorsal root ganglion (DRG) neurons, the axons of which degenerate in small fiber neuropathy, leading to various neuropathic manifestations. Mechanisms underlying positive and negative symptoms
The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells
Akeno-Stuart N, et al.
Cancer Research, 67(14), 6956-6964 (2007)
Pharmacological profile of the FLT3-Tyrosine Kinase Inhibitor AST487
Roesel JL, Bold G, Brueggen J, Fabbro D, Floersheimer A, Jensen-Rugaard M, Ruetz S, et al.
Proceedings of the American Association For Cancer Research, 46 (2005)
Nagako Akeno-Stuart et al.
Cancer research, 67(14), 6956-6964 (2007-07-20)
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, a N,N'-diphenyl urea with an IC(50) of 0.88 mumol/L on RET kinase, inhibited RET
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