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Chemical Structure : TAS-116
CAS No.: 1260533-36-5
Catalog No.: PC-61958Not For Human Use, Lab Use Only.
TAS-116 (Pimitespib, TAS116) is a novel potent, selective, orally available HSP90α/β inhibitor with Ki of 34.7, 21.3, >50,000, and >50,000 nM for HSP90α, HSP90β, GRP94, and TRAP1, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $258 | In stock | |
| 50 mg | $458 | In stock | |
| 100 mg | $758 | In stock | |
| 250 mg | $1180 | In stock | |
| 1 g | Get quote |
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TAS-116 (Pimitespib, TAS116) is a novel potent, selective, orally available HSP90α/β inhibitor with Ki of 34.7, 21.3, >50,000, and >50,000 nM for HSP90α, HSP90β, GRP94, and TRAP1, respectively.
TAS-116 induces cytotoxicity selectively and potently in MM cell lines and patient MM cells, without toxicity in normal PBMNCs.
TAS-116 potently targets HSP90 client proteins including C-Raf and MEK1/2.
TAS-116 also inhibits upregulation of HSP27 and overcomes 17-AAG resistance mechanisms in MM cells.
TAS-116 demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models.
| M.Wt | 454.538 | |
| Formula | C25H26N8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
3-Ethyl-4-[3-(1-methylethyl)-4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-1H-pyrazolo[3,4-b]pyridin-1-yl]benzamide |
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1. Suzuki R, et al. Leukemia. 2015 Feb;29(2):510-4.
2. Ohkubo S, et al. Mol Cancer Ther. 2015 Jan;14(1):14-22.
3. Suzuki R, et al. PLoS One. 2015 Dec 2;10(12):e0143847.
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