Name | GSK 1838705 |
---|---|
Supplier | Tocris Bioscience |
Catalog | 5110 |
Prices | $245.00, $1,005.00 |
Sizes | 10 mg, 50 mg |
Function Type | Inhibitor |
Cas Number | 1116235-97-2 |
Chemical Name | 2-[[2-[[1-[(Dimethylamino)ethanoyl]-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide |
Formula | C27H29FN8O3 |
Molecular Weight | 532.57 |
Purity | >98 % |
Description | Potent insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1R) inhibitor (IC 50 values are 1.6 and 2 nM, respectively). Also inhibits anaplastic lymphoma kinase (ALK) (IC 50 = 0.5 nM). Displays > 800-fold selectivity for IR, IGFR1 and ALK over a panel of 44 kinases including JNK. Blocks proliferation of cancer cell lines in vitro , and causes complete regression of ALK-dependent tumors in vivo . Orally bioavailable. |
Supplier Page | Shop |
Chamberlain SD, Redman AM, Wilson JW, Deanda F, Shotwell JB, Gerding R, Lei H, Yang B, Stevens KL, Hassell AM, Shewchuk LM, Leesnitzer MA, Smith JL, Sabbatini P, Atkins C, Groy A, Rowand JL, Kumar R, Mook RA Jr, Moorthy G, Patnaik S. Bioorg Med Chem Lett. 2009 Jan 15;19(2):360-4.
Sabbatini P, Korenchuk S, Rowand JL, Groy A, Liu Q, Leperi D, Atkins C, Dumble M, Yang J, Anderson K, Kruger RG, Gontarek RR, Maksimchuk KR, Suravajjala S, Lapierre RR, Shotwell JB, Wilson JW, Chamberlain SD, Rabindran SK, Kumar R. Mol Cancer Ther. 2009 Oct;8(10):2811-20.
Gao M, Liang J, Lu Y, Guo H, German P, Bai S, Jonasch E, Yang X, Mills GB, Ding Z. Oncogene. 2014 Feb 6;33(6):745-55.