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Merck
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重要文件

SML3675

Sigma-Aldrich

GSK1904529A

≥98% (HPLC)

同義詞:

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

經驗公式(希爾表示法):
C44H47F2N9O5S
CAS號碼:
分子量::
851.96
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.21

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear (Warmed)

儲存溫度

-10 to -25°C

SMILES 字串

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 密鑰

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).
Orally active, potent and selective insulin-like growth factor-1 receptor (IGF-1R) & insulin receptor (InsR, IR) inhibitor in vitro and in vivo.

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


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分析證明 (COA)

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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
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
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

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