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Merck
CN

SML3156

Sigma-Aldrich

ALW-II-41-27

≥98% (HPLC)

别名:

ALW-II-247, N-(5-(4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenylcarbamoyl)-2-methylphenyl)-5-(thiophen-2-yl)nicotinamide, N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-[[[5-(2-thienyl)-3-pyridinyl]carbonyl]amino]benzamide

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关于此项目

经验公式（希尔记法）:
C32H32F3N5O2S
化学文摘社编号:
1186206-79-0
分子量:
607.69
MDL编号:
MFCD25372028
UNSPSC代码:
12352200
NACRES:
NA.77

主要文件

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质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

O=C(NC1=CC=C(CN2CCN(CC)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(NC(C4=CC(C5=CC=CS5)=CN=C4)=O)=C3

InChI

1S/C32H32F3N5O2S/c1-3-39-10-12-40(13-11-39)20-23-8-9-26(17-27(23)32(33,34)35)37-30(41)22-7-6-21(2)28(16-22)38-31(42)25-15-24(18-36-19-25)29-5-4-14-43-29/h4-9,14-19H,3,10-13,20H2,1-2H3,(H,37,41)(H,38,42)

InChI key

HYWXBDQAYLPMIX-UHFFFAOYSA-N

生化/生理作用

ALW-II-41-27 is an RG-25 (RG25) structural analog that exhibits enhanced type II kinase inhibitor activity against ephrin type-A receptor 2/EphA2/ECK (IC50 = 11 nM vs 770 nM with NG25) by targeting the ATP-binding pocket and an allosteric site next to the “DFG” motif. ALW-II-41-27 inhibits constitutive and ephrin A1-induced EphA2 tyrosine phosphorylation (0.1-1 μM; H358), effectively suppressing EphA2-dependent cancer survival in vitro (0.1-1 μM for 72 hrs; NSCLC) and xenograft tumor growth in mice in vivo (15-30 mg/kg b.i.d. i.p.; H358 NSCLC & A375 melanoma). Note: ALW-II-41-27 and RG-25 (RG25) display very similar kinase-targeting profiles with EphA2 being a notable exception, RG25 can therefore serve as a control for ALW-II-41-27 when probing EphA2-mediated cellular functions.
Type II ATP-competitive EphA2 inhibitor that inhibits EphA2 tyrosine phosphorylation and EphA2-dependent NSCLC survival 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
0000136703
0000136704
0000134137

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Katherine R Amato et al.
The Journal of clinical investigation, 124(5), 2037-2049 (2014-04-10)
Genome-wide analyses determined previously that the receptor tyrosine kinase (RTK) EPHA2 is commonly overexpressed in non-small cell lung cancers (NSCLCs). EPHA2 overexpression is associated with poor clinical outcomes; therefore, EPHA2 may represent a promising therapeutic target for patients with NSCLC.
Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer.
Terai, et al.
ACS chemical biology, 10, 2687-2696 (2018)
Katherine R Amato et al.
Cancer research, 76(2), 305-318 (2016-01-09)
Despite the success of treating EGFR-mutant lung cancer patients with EGFR tyrosine kinase inhibitors (TKI), all patients eventually acquire resistance to these therapies. Although various resistance mechanisms have been described, there are currently no FDA-approved therapies that target alternative mechanisms
Yongmun Choi et al.
Bioorganic & medicinal chemistry letters, 19(15), 4467-4470 (2009-06-26)
The Eph family of receptor tyrosine kinases has drawn growing attention due to their role in regulating diverse biological phenomena. However, pharmacological interrogation of Eph kinase function has been hampered by a lack of potent and selective Eph kinase inhibitors.
W Song et al.
Oncogene, 36(40), 5620-5630 (2017-06-06)
Basal-like/triple-negative breast cancers (TNBCs) are among the most aggressive forms of breast cancer, and disproportionally affects young premenopausal women and women of African descent. Patients with TNBC suffer a poor prognosis due in part to a lack of molecularly targeted
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