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Merck
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文件

SML2363

Sigma-Aldrich

AST487

≥98% (HPLC)

同義詞:

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

經驗公式（希爾表示法）:
C26H30F3N7O2
CAS號碼:
630124-46-8
分子量：:
529.56
MDL號碼:
MFCD11983171
分類程式碼代碼:
12352200

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

−20°C

SMILES 字串

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 密鑰

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析證明 (COA)

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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)
Ellen Weisberg et al.
Blood, 112(13), 5161-5170 (2008-09-30)
An attractive target for therapeutic intervention is constitutively activated, mutant FLT3, which is expressed in a subpopulation of patients with acute myelocyic leukemia (AML) and is generally a poor prognostic indicator in patients under the age of 65 years. PKC412
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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