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Merck
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Documentos

SML3675

Sigma-Aldrich

GSK1904529A

≥98% (HPLC)

Sinônimo(s):

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

Fórmula empírica (Notação de Hill):
C44H47F2N9O5S
Número CAS:
Peso molecular:
851.96
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.21

Nível de qualidade

Ensaio

≥98% (HPLC)

forma

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear (Warmed)

temperatura de armazenamento

-10 to -25°C

Ações bioquímicas/fisiológicas

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).

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


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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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