TAS-116, inhibitor

TAS-116

Cat. Num. AAA5755588

• Purity: 98.00%
• Synonyms: TAS-116; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 125mg/mL (275.01mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C25H26N8O
• SMILES: CCc1cc(ccc1-n1nc(C(C)C)c2c(ccnc12)-n1cnc(c1)-c1cnn(C)c1)C(N)=O
• CAS Number: 1260533-36-5
• Target & IC50: HSP90alpha: ic50 34.7nM (ki); HSP90beta: ic50 21.3nM (ki)
• In Vitro: TAS-116 is orally absorbed and has a bioavailability of almost 100% in mice, and 69.0% in rats. TAS-116 has moderate terminal elimination half-life (t1/2=8.2 h, 2.5 h, 4.4 h and 2.2 h for mouse (3.6mg/kg, p.o.), mouse (7.1mg/kg, p.o.), mouse (14.0mg/kg, p.o.), rat (4mg/kg, p.o.)). TAS-116 is more rapidly eliminated from retina (t1/2=3.4 hours) than the other HSP90 inhibitors (t1/2=7.1-19.1 hours). TAS-116 is distributed less in retina than in plasma in rats; consequently, TAS-116 does not produce any detectable photoreceptor injury. TAS-116 triggers enhanced in vivo anti-MM activities, both alone and in combination with Bortezomib (BTZ), with a favorable safety profile. TAS-116 (12.0mg/kg, p.o., 14 days) displays antitumor activity without inducing eye injury in rats. Mice treated with TAS-116 (10mg/kg and 15mg/kg, orally, 38 days), BTZ, or TAS-116 plus BTZ show significantly enhance growth inhibition versus the vehicle control group. Median overall survival of treated animals (TAS-116, orally, 10mg/kg=33 days, 15mg/kg=37 days, BTZ=36 days, and the combination=56.5 days) is significantly longer than vehicle control. The favorable pharmacokinetic profile of TAS-116 is reflected in its dose-dependent antitumor activity; the T/C (tumor volume of TAS-116-treated mice vs. vehicle-treated mice) is 47%, 21%, and 9% for doses of 3.6mg/kg, 7.1mg/kg, and 14.0mg/kg, respectively [1][2].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for TAS-116, inhibitor

TAS-116 is an ATP-competitive and highly specific HSP90alpha/HSP90beta inhibitor (Kis: 34.7nM and 21.3nM, respectively).

Product Categories/Family for TAS-116, inhibitor

Cytoskeletal Signaling; HSP; Metabolism

References

Ohkubo S, et al. TAS-116, a highly selective inhibitor of heat shock protein 90alpha and beta, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models. Mol Cancer Ther. 2015 Jan;14(1):14-22.
Ohkubo S, et al. TAS-116, a highly selective inhibitor of heat shock protein 90alpha and beta, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models. Mol Cancer Ther. 2015 Jan;14(1):14-22.
Suzuki R, et al. Anti-tumor activities of selective HSP90alpha/beta inhibitor, TAS-116, in combination with bortezomib in multiple myeloma. Leukemia. 2015 Feb;29(2):510-4.
Suzuki R, et al. Anti-tumor activities of selective HSP90alpha/beta inhibitor, TAS-116, in combination with bortezomib in multiple myeloma. Leukemia. 2015 Feb;29(2):510-4.
Utsugi T. New challenges and inspired answers for anticancer drug discovery and development. Jpn J Clin Oncol. 2013 Oct;43(10):945-53.
Utsugi T. New challenges and inspired answers for anticancer drug discovery and development. Jpn J Clin Oncol. 2013 Oct;43(10):945-53.