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Merck
CN

SML3675

GSK1904529A

≥98% (HPLC)

Synonym(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

Empirical Formula (Hill Notation):
C44H47F2N9O5S
CAS Number:
1089283-49-7
Molecular Weight:
851.96
UNSPSC Code:
12352200
NACRES:
NA.21
MDL number:
MFCD17010271

Key Documents

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Product Name

GSK1904529A, ≥98% (HPLC)

SMILES string

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

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

-10 to -25°C

Quality Level

100

Related Categories

Biochem/physiol Actions

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000259290
0000259296
0000246069
0000246069
0000259290

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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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