1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP
  3. TAS-116

TAS-116 

Cat. No.: HY-15785 Purity: 98.96%
Handling Instructions

TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.

For research use only. We do not sell to patients.

TAS-116 Chemical Structure

TAS-116 Chemical Structure

CAS No. : 1260533-36-5

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10 mM * 1 mL in DMSO USD 94 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 145 In-stock
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100 mg USD 940 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94[1]. TAS-116 demonstrates less ocular toxicity[2].

IC50 & Target[1]

HSP90α

34.7 nM (Ki)

HSP90β

21.3 nM (Ki)

In Vitro

TAS-116 binds not only to the conventional-binding pockets as existing Hsp-90 inhibitors, but also to a novel-binding pocket. Such a unique binding mode makes TAS-116 highly specific for Hsp-90α/β without inhibiting other Hsp-90 family proteins such as GRP94 in endoplasmic reticulum or TRAP-1 in mitochondria[3].
TAS-116 (0-5 μM, 48 hours) inhibits human retinal pigment epithelial ARPE-19 cell lines and NCI-H929 MM cells growth[2].
More significant degradation of p-C-Raf and p-MEK1/2, HSP90 client proteins and key RAS/RAF/MEK pathway regulators, is triggered by TAS-116 (0.125-1 μM, 24 hours) than 17-AAG in INA6 and NCI-H929 MM cells[2].

Cell Viability Assay[2]

Cell Line: Human retinal pigment epithelial ARPE-19 cell lines and NCI-H929 MM cells
Concentration: 0-5 μM
Incubation Time: 48 hours
Result: Inhibited NCI-H929 MM cells growth with an IC50 of 0.35 μM.

Western Blot Analysis[2]

Cell Line: MM cell lines INA6 and NCI-H929 cells
Concentration: 0.125-1 μM
Incubation Time: 24 hours
Result: Targeted potently HSP90 client proteins including C-Raf and MEK1/2; as well as inhibited upregulation of HSP27 and overcomes 17-AAG resistance mechanisms.
In Vivo

TAS-116 (12.0 mg/kg, p.o., 14 days) shows antitumor activity without inducing eye injury in rats. TAS-116 is distributed less in retina than in plasma in rats; consequently, TAS-116 does not produce any detectable photoreceptor injury[1]. TAS-116 triggers enhanced in vivo anti-MM activities, both alone and in combination with Bortezomib (BTZ), with a favorable safety profile. Mice treated with TAS-116 (10 mg/kg and 15 mg/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, 10 mg/kg=33 days, 15 mg/kg=37 days, BTZ=36 days, and the combination=56.5 days) is significantly longer than vehicle control[2].
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 3.6 mg/kg, 7.1 mg/kg, and 14.0 mg/kg, respectively. 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 (3.6 mg/kg, p.o.), mouse (7.1 mg/kg, p.o.), mouse (14.0 mg/kg, p.o.), rat (4 mg/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)[1].

Animal Model: Male F344 nude rats (6 weeks old) with established NCI-H1975 xenografts (6 weeks old)[1]
Dosage: 12.0 mg/kg
Administration: Oral administration; daily; two weeks
Result: Led to tumor shrinkage. Showed antitumor activity without inducing eye injury in rats and did not cause ocular toxicity at the effective dose in the NCI-H1975 rat xenograft model.
Animal Model: CB17 SCID mice (48-54 days old) with murine xenograft model[2]
Dosage: 10 and 15 mg/kg
Administration: Oral administration; 5 days a week; for 28 days
Result: Enhanced significantly growth inhibition versus the vehicle control group. The delay in tumor growth was greater in the combination-treated group compared with either monotherapy cohort.
Animal Model: Mice, Rats, and Dogs[1]
Dosage: 3.0 mg/kg for dogs, 4.0 mg/kg for rats, 3.6, 7.1 and 14.0 mg/kg for mice
Administration: Oral administration; daily; 20 days
Result: Absorbed orally and had a bioavailability of almost 100% in mice, 69.0% in rats, and 73.9% in dogs without special formulation.
Clinical Trial
Molecular Weight

454.53

Formula

C₂₅H₂₆N₈O

CAS No.

1260533-36-5

SMILES

O=C(N)C1=CC=C(N2N=C(C(C)C)C3=C(N4C=C(C5=CN(C)N=C5)N=C4)C=CN=C32)C(CC)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (275.01 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2001 mL 11.0004 mL 22.0007 mL
5 mM 0.4400 mL 2.2001 mL 4.4001 mL
10 mM 0.2200 mL 1.1000 mL 2.2001 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.58 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.58 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.58 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TAS-116TAS116TAS 116HSPHeat shock proteinsInhibitorinhibitorinhibit

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TAS-116
Cat. No.:
HY-15785
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