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Merck
CN

SML3675

Sigma-Aldrich

GSK1904529A

≥98% (HPLC)

别名:

GSK 1904529, GSK 1904529A, GSK 4529, GSK-1904529, GSK-1904529A, GSK-4529, GSK1904529, GSK4529, N-(2,6-Difluorophenyl)-5-[3-[2-[[5-ethyl-2-(methyloxy)-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]imidazo[1,2-a]pyridin-2-yl]-2-(methyloxy)benzamide

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About This Item

经验公式(希尔记法):
C44H47F2N9O5S
分子量:
851.96
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.21

质量水平

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear (Warmed)

储存温度

-10 to -25°C

SMILES字符串

Fc1c(c(ccc1)F)NC(=O)c2c(ccc(c2)c3nc4[n](c3c5nc(ncc5)Nc6c(cc(c(c6)CC)N7CCC(CC7)N8CCN(CC8)[S](=O)(=O)C)OC)cccc4)OC

InChI key

MOSKATHMXWSZTQ-UHFFFAOYSA-N

生化/生理作用

GSK1904529A is an orally active, potent and selective insulin-like growth factor-1 receptor and insulin receptor inhibitor (IGF-1R/IR IC50 = 27/25 nM; IC50 ≥3.2 μM/35 other kinases) that blocks cellular receptor autophosphorylation and downstream signaling. GSK1904529A inhibits IGF-1R-dependent proliferation in cancer cultures (IC50 in nM = 81-165/multiple myeloma, 35-62/Ewing′s sarcoma, 43/Askin’s tumor SK-N-MC, 104-124/colon cancer, 137-189/breast cancer) and suppresses the growth of human tumor xenografts in mice in vivo (30 mg/kg via qd. or bid. po.; HT29, BxPC3, COLO 205, NIH-3T3-LISN).

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number

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Peter Sabbatini et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 15(9), 3058-3067 (2009-04-23)
Dysregulation of the insulin-like growth factor-I receptor (IGF-IR) signaling pathway has been implicated in the development of many types of tumors, including prostate, colon, breast, pancreatic, ovarian, and sarcomas. Agents that inhibit IGF-IR activity may be useful in treatment of
Pranav Gupta et al.
Journal of cellular biochemistry, 118(10), 3260-3267 (2017-03-08)
Overexpression of multidrug-resistant efflux transporters is one of the major causes of chemotherapy failure. MRP1, a 190 kDa efflux transporter, confers resistance to a wide of range of chemotherapeutic drugs. Here we study the cellular effects of GSK1904529A in reversing MRP1-mediated
Chengyu Li et al.
Biology of reproduction, 102(1), 116-132 (2019-08-23)
As the follicle develops, the thickening of the granulosa compartment leads to progressively deficient supply of oxygen in granulosa cells (GCs) due to the growing distances from the follicular vessels. These conditions are believed to cause hypoxia in GCs during

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