TAS-116
- CAS No.
- 1260533-36-5
- Chemical Name:
- TAS-116
- Synonyms
- TAS-116;Pimitespib;TAS 116;TAS116;Des-iPr-TAS-116;Pimitespib (TAS-116);inhibit,HSP,TAS 116,TAS116,Pimitespib,Heat shock proteins,Inhibitor;3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide;Benzamide, 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]-
- CBNumber:
- CB22716365
- Molecular Formula:
- C25H26N8O
- Molecular Weight:
- 454.53
- MDL Number:
- MFCD28502196
- MOL File:
- 1260533-36-5.mol
- MSDS File:
- SDS
| Boiling point | 661.7±55.0 °C(Predicted) |
|---|---|
| Density | 1.36±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMSO: soluble |
| form | A solid |
| pka | 15.43±0.50(Predicted) |
| FDA UNII | PLO044MUDZ |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
TAS-116 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0009135 | TAS-116 98.96% | 1260533-36-5 | 5mg | $85 | 2021-12-16 | Buy |
| American Custom Chemicals Corporation | INB0004535 | TAS-116 95.00% | 1260533-36-5 | 5MG | $503.05 | 2021-12-16 | Buy |
| ChemScene | CS-0009135 | TAS-116 98.96% | 1260533-36-5 | 50mg | $530 | 2021-12-16 | Buy |
| ChemScene | CS-0009135 | TAS-116 98.96% | 1260533-36-5 | 100mg | $940 | 2021-12-16 | Buy |
| ChemScene | CS-0009135 | TAS-116 98.96% | 1260533-36-5 | 10mg | $1450 | 2021-12-16 | Buy |
TAS-116 Chemical Properties,Uses,Production
Biological Activity
TAS-116 is a novel small molecule inhibitor of HSP90 with Ki values of 34.7 nmol/L and 21.3 nmol/L for HSP90α and HSP90β, respectively. It does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L).
in vitro
TAS-116 is a selective inhibitor of HSP90α and HSP90β in the cytoplasm, but has no inhibitory effect on endoplasmic reticulum GRP94 or mitochondrial TRAP1. Treatment of HCT116 cells with 0.3 μM of TAS-1116 for 8 hours resulted in a decrease in DDR1 levels and induction of HSP70.
in vivo
In a mouse model with human xenograft tumors, oral administration of TAS-116 induced tumor shrinkage accompanied by depletion of HSP90. In a rat model, TAS-116 was more distributed in subcutaneously xenografted NCI-H1975 non-small cell lung cancer tumors than in the retina. TAS-116 was also active in orthotopically transplanted NCI-H1975 lung tumors.
target
| Target | Value |
| HSP90β (Cell-free assay) | 21.3 nM(Ki) |
| HSP90α (Cell-free assay ) | 34.7 nM(Ki) |
TAS-116 Preparation Products And Raw materials
Raw materials
Preparation Products
TAS-116 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| NCE Biomedical Co.,Ltd. | 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 | China | 1494 | 55 |