GSK-1904529a
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MedKoo CAT#: 401480

CAS#: 1089283-49-7

Description: GSK-1904529A, also known as GSK 4529, is an IGF-1R Inhibitor, is is a promising candidate for therapeutic use in IGF-IR–dependent tumors. GSK1904529A selectively inhibits IGF-IR and IR with IC50s of 27 and 25 nmol/L, respectively. GSK1904529A blocks receptor autophosphorylation and downstream signaling, leading to cell cycle arrest. It inhibits the proliferation of cell lines derived from solid and hematologic malignancies, with multiple myeloma and Ewing's sarcoma cell lines being most sensitive. Oral administration of GSK1904529A decreases the growth of human tumor xenografts in mice, consistent with a reduction of IGF-IR phosphorylation in tumors. Despite the potent inhibitory activity of GSK1904529A on IR in vitro and in vivo , minimal effects on blood glucose levels are observed in animals at doses that show significant antitumor activity. (source: Clin Cancer Res May 1, 2009 15; 3058 )


Chemical Structure

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GSK-1904529a
CAS# 1089283-49-7

Theoretical Analysis

MedKoo Cat#: 401480
Name: GSK-1904529a
CAS#: 1089283-49-7
Chemical Formula: C44H47F2N9O5S
Exact Mass: 851.33889
Molecular Weight: 851.96309
Elemental Analysis: C, 62.03; H, 5.56; F, 4.46; N, 14.80; O, 9.39; S, 3.76

Price and Availability

Size Price Availability Quantity
10.0mg USD 340.0 2 Weeks
25.0mg USD 575.0 2 Weeks
50.0mg USD 880.0 2 Weeks
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Synonym: GSK 4529; GSK4529; GSK-4529; GSK1904529a; GSK 1904529; GSK-1904529a .

IUPAC/Chemical Name: 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

InChi Key: MOSKATHMXWSZTQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C44H47F2N9O5S/c1-5-28-26-35(38(60-3)27-36(28)53-19-15-30(16-20-53)52-21-23-54(24-22-52)61(4,57)58)49-44-47-17-14-34(48-44)42-40(50-39-11-6-7-18-55(39)42)29-12-13-37(59-2)31(25-29)43(56)51-41-32(45)9-8-10-33(41)46/h6-14,17-18,25-27,30H,5,15-16,19-24H2,1-4H3,(H,51,56)(H,47,48,49)

SMILES Code: O=C(NC1=C(F)C=CC=C1F)C2=CC(C3=C(C4=NC(NC5=CC(CC)=C(N6CCC(N7CCN(S(=O)(C)=O)CC7)CC6)C=C5OC)=NC=C4)N8C=CC=CC8=N3)=CC=C2OC

Appearance: Solid powder

Purity: >95% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 851.96309 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Sabbatini P, Rowand JL, Groy A, Korenchuk S, Liu Q, Atkins C, Dumble M, Yang J, Anderson K, Wilson BJ, Emmitte KA, Rabindran SK, Kumar R. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I eceptor tyrosine kinase. Clin Cancer Res. 2009 May 1;15(9):3058-67. Epub 2009 Apr 21. PubMed PMID: 19383820.



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