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MedKoo Biosciences/GSK-1904529a/401480/500mg

  
  2024-04-28
  
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 Ewings 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 )

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

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

Technical Data

Appearance: Solid powder

Purity: >98% (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).

Harmonized System Code: 293490

Additional Information

       

References

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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