A dual inhibitor of InsR and IGF-1R kinases
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GSK1904529A

Item No. 29155

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2,6-difluorophenyl)-5-[3-[2-[[5-ethyl-2-methoxy-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]imidazo[1,2-a]pyridin-2-yl]-2-methoxy-benzamide
CAS Number
1089283-49-7
Molecular Formula
C44H47F2N9O5S
Formula Weight
852.0
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF:PBS (pH 7.2): 0.8 mg/ml
SMILES
O=C(NC1=C(F)C=CC=C1F)C2=CC(C3=C(C4=NC(NC5=C(OC)C=C(N6CCC(N7CCN(S(C)(=O)=O)CC7)CC6)C(CC)=C5)=NC=C4)N8C=CC=CC8=N3)=CC=C2OC
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)
InChi Key
MOSKATHMXWSZTQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

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    10 mg

    $236

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    25 mg

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    Product Description

    GSK1904529A is a dual inhibitor of the insulin receptor (InsR) and insulin-like growth factor 1 receptor (IGF-1R) kinases (IC50s = 25 and 27 nM, respectively, in a cell-free assay).1 It selectively inhibits InsR and IGF-1R kinases over a panel of 45 serine/threonine and tyrosine kinases (IC50s = >1 µM for all). GSK1904529A decreases proliferation of 13 cancer cell lines, including multiple myeloma, sarcoma, colon, and breast cancer cells, with IC50 values ranging from 35 to 189 nM in a panel of 35 cell lines. It reduces tumor growth in NIH3T3-LISN, COLO 205, HT-29, and BxPC3 mouse xenograft models when administered at a dose of 30 mg/kg for 21 days.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sabbatini, P., Rowand, J.L., Groy, A., et al. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Clin. Cancer Res. 15(9), 3058-3067 (2009).