TAS0728
- CAS No.
- 2088323-16-2
- Chemical Name:
- TAS0728
- Synonyms
- AS0728;TAS0728;TPC-107;TAS0728, 10 mM in DMSO;TAS0728;TAS-0728;TAS 0728;TAS 0728,Inhibitor,EGFR,ErbB-1,inhibit,TAS0728,HER1,TAS-0728,Epidermal growth factor receptor;(R)-1-(1-Acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide;1H-Pyrazolo[3,4-d]pyrimidine-3-carboxamide, 4-amino-N-[4-[2-(dimethylamino)-2-oxoethyl]-2,3-dimethylphenyl]-1-[(3R)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl]-
- CBNumber:
- CB55417169
- Molecular Formula:
- C26H32N8O3
- Molecular Weight:
- 504.58
- MDL Number:
- MFCD31813813
- MOL File:
- 2088323-16-2.mol
- MSDS File:
- SDS
- TDS File:
- TDS
TAS0728 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 33528 | TAS 0728 ≥98% | 2088323-16-2 | 1mg | $95 | 2026-04-30 | Buy |
| Cayman Chemical | 33528 | TAS 0728 ≥98% | 2088323-16-2 | 5mg | $370 | 2026-04-30 | Buy |
| Cayman Chemical | 33528 | TAS 0728 ≥98% | 2088323-16-2 | 10mg | $601 | 2026-04-30 | Buy |
| Cayman Chemical | 33528 | TAS 0728 ≥98% | 2088323-16-2 | 25mg | $922 | 2026-04-30 | Buy |
| Biosynth | NID32316 | TAS0728 | 2088323-16-2 | 10mg | $779.6 | 2026-06-04 | Buy |
TAS0728 Chemical Properties, Uses, Production
Uses
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors[1].
in vivo
TAS0728 reveals the sustained and targeted inhibition of phosphorylation of HER2, HER3, AKT and ERK. TAS0728 also shows the ability of tumor regression and low toxicity[1].
| Animal Model: | Male nude mice |
| Dosage: | 7.5, 15, 30 and 60 mg/kg |
| Administration: | Oral gavage; 7.5, 15, 30 and 60 mg/kg a day;14 days |
| Result: | Rapidly eliminated within 24 hours. |
| Animal Model: | Mice bearing NCI-N87 xenografts |
| Dosage: | 60 mg/kg |
| Administration: | Oral gavage; 60 mg/kg a day; 14 days |
| Result: | Revealed sustained target inhibition of HER2, HER3, AKT and ERK. |
| Animal Model: | Mice with NCI-N87 HER2–amplified human gastric cancer |
| Dosage: | 7.5, 15, 30 and 60 mg/kg |
| Administration: | Oral gavage; 7.5, 15, 30 and 60 mg/kg a day; 14 days |
| Result: | Well tolerated in all mice. Significant tumor regression was observed in mice treated with 60 mg/kg/day. |
| Animal Model: | NCI-N87 peritoneal dissemination model |
| Dosage: | 30 and 60 mg/kg |
| Administration: | Oral gavage; 30and 60 mg/kg a day; 120 days |
| Result: | No evident toxicity, including diarrhea and body weight loss in the long-term dosing of TAS0728. |
IC 50
HER4: 8.5 nM (IC50); HER2: 13 nM (IC50); EGFR: 65 nM (IC50); BMX: 4.9 nM (IC50); BLK: 31 nM (IC50); JAK3: 33 nM (IC50); SLK: 25 nM (IC50); LOK: 86 nM (IC50)
References
[1] Irie H, et al. TAS0728, A Covalent-binding, HER2-selective Kinase Inhibitor Shows Potent Antitumor Activity in Preclinical Models. Molecular cancer therapeutics. 2019;18(4):733-42. Epub 2019/02/23. DOI:10.1158/1535-7163.MCT-18-1085
TAS0728 Preparation Products And Raw materials
Raw materials
Preparation Products
TAS0728 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185 | sales-cpd@caerulumpharma.com | China | 3493 | 58 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4859 | 55 | |
| Lianyungang TengFa Biological Technology Co. Ltd | 0518-85475186 18705131893 | wang666xt@163.com | China | 351 | 55 |
| Shanghai Beckham Medical Technology Co., Ltd | 13816613772 | huahero21@sina.com | China | 2994 | 55 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9799 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| ShangHai Biochempartner Co.,Ltd | 177-54423994 17754423994 | 2853530910@QQ.com | China | 8000 | 62 |
| Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9718 | 58 |
| BOC Sciences | 16314854226; +8616314854226 | inquiry@bocsci.com | United States | 19852 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
