| Name | EC 144 |
|---|---|
| Supplier | Tocris Bioscience |
| Catalog | 5245 |
| Prices | $235.00 |
| Sizes | 10 mg |
| Function Type | Inhibitor |
| Cas Number | 911397-80-3 |
| Chemical Name | 5-[2-Amino-4-chloro-7-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-2-methyl-4-pentyn-2-ol |
| Formula | C21H24ClN5O2 |
| Molecular Weight | 413.9 |
| Purity | >98 % |
| Description | High affinity, potent and selective Hsp90 inhibitor (K i = 0.2 nM and IC 50 = 1.1 nM). Exhibits selectivity for Hsp90 over Grp94 and TRAP1 (K i values are 61 and 255 nM respectively) and has no effect (IC 50 >10 μ M) against a panel of 285 kinases. Degrades Her-2 in MCF-7 breast cancer cells (EC 50 = 14 nM). Blocks tumor growth and induces partial tumor regression in an N87 gastric tumor mouse model. Also inhibits LPS-induced TNF α release in an LPS shock mouse model and suppresses disease development in a rat model of collagen-induced arthritis. Exhibits <20-fold efficacy over BIIB 021 (Cat. No. 4608) in mice. Orally available and brain penetrant. |
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Yun TJ, Harning EK, Giza K, Rabah D, Li P, Arndt JW, Luchetti D, Biamonte MA, Shi J, Lundgren K, Manning A, Kehry MR. J Immunol. 2011 Jan 1;186(1):563-75.
Shi J, Van de Water R, Hong K, Lamer RB, Weichert KW, Sandoval CM, Kasibhatla SR, Boehm MF, Chao J, Lundgren K, Timple N, Lough R, Ibanez G, Boykin C, Burrows FJ, Kehry MR, Yun TJ, Harning EK, Ambrose C, Thompson J, Bixler SA, Dunah A, Snodgrass-Belt P, Arndt J, Enyedy IJ, Li P, Hong VS, McKenzie A, Biamonte MA. J Med Chem. 2012 Sep 13;55(17):7786-95.