Pimitespib (TAS-116) | HSP90α/β inhibitor

Chemical Structure : TAS-116

CAS No.: 1260533-36-5

TAS-116 (Pimitespib, TAS 116, TAS116)

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
10 mg	$98	In stock
25 mg	$158	In stock
50 mg	$258	In stock
100 mg	$398	In stock
250 mg		Get quote

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Biological Activity

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.

Physicochemical Properties

M.Wt	454.538
Formula	C25H26N8O
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
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

References

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.

TAS-116 (Pimitespib, TAS 116, TAS116)

Biological Activity

Physicochemical Properties

References

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