TAK-285
- CAS No.
- 871026-44-7
- Chemical Name:
- TAK-285
- Synonyms
- CS-255;TAK-285;TAK-285(TAK 285);TAK-285 USP/EP/BP;N-(2-(4-(3-Chloro-4-(3-(trifluoromethyl)phenoxy)phenylamino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl)e;N-[2-[4-[[3-Chloro-4-[3-(trifluoromethyl)phenoxy]phenyl]amino]-5H-pyrrolo[3,2-d]pyrimidin-5-yl]ethyl]-3-hydroxy-3-methylbutanamide;Butanamide, N-[2-[4-[[3-chloro-4-[3-(trifluoromethyl)phenoxy]phenyl]amino]-5H-pyrrolo[3,2-d]pyrimidin-5-yl]ethyl]-3-hydroxy-3-methyl-
- CBNumber:
- CB72621152
- Molecular Formula:
- C26H25ClF3N5O3
- Molecular Weight:
- 547.96
- MDL Number:
- MFCD22124520
- MOL File:
- 871026-44-7.mol
- MSDS File:
- SDS
| Melting point | 167-169℃ |
|---|---|
| Boiling point | 705.5±60.0 °C(Predicted) |
| Density | 1.39 |
| storage temp. | Store at -20°C |
| solubility | ≥27.4 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| form | solid |
| pka | 14.56±0.29(Predicted) |
| FDA UNII | 70CCB438L6 |
TAK-285 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0774 | TAK-285 98.04% | 871026-44-7 | 5mg | $90 | 2021-12-16 | Buy |
| ChemScene | CS-0774 | TAK-285 98.04% | 871026-44-7 | 10mg | $150 | 2021-12-16 | Buy |
| AK Scientific | SYN1153 | TAK-285 | 871026-44-7 | 1mg | $185 | 2021-12-16 | Buy |
| ApexBio Technology | A8528 | TAK-285 | 871026-44-7 | 5mg | $189 | 2021-12-16 | Buy |
| Biosynth Carbosynth | FT103851 | TAK 285 | 871026-44-7 | 10mg | $225 | 2021-12-16 | Buy |
TAK-285 Chemical Properties,Uses,Production
Uses
TAK-285 is a novel dual HER2 and EGFR inhibitor with IC50 of 17 nM and 23 nM, respectively.
Biological Activity
tak-285 is a potent inhibitor of her2 and egfr with ic50 value of 17 nm and 23 nm, respectively [1].egfr (epidermal growth factor receptor) and her2 are members of erbb family of receptors and play an important role in stimulating its intrinsic intracellular protein-tyrosine kinase activity. it has been shown that the over-expressions of her-2 and egfr are correlated with a variety of cancers and thus be regarded as promising target in clinic [2].tak-285 is a selective her2 and egfr inhibitor and has a different selectivity with the reported her inhibitor ast-6. when tested with a panel of breast cancer cell lines, cells over-expressed her2 (bt-474, nci-n87, sk-br-3, calu-3, and mda-mb-453) or egfr (a-431) were more sensitive to tak-285 treatment while normal expressed cell line (mrc-5) was less sensitive [1]. [3].in rat model with 4-1st (over-express her2) or a-431 (over-express egfr) subcutaneous xenograft, administration of tak-285 caused significant reduction of tumor growth with t/c values of 14% and 13%, respectively, at a dose of 12.5 mg/kg, compared with control group [1]. in a panel of human breast cancer cell lines expressing egfr, her2, her3, and her4, administration of tak-285 significantly inhibited cell proliferation in a dose-dependent manner with ic50 values range from 0.011 to 17 μm [3].it is also reported that tak-285 inhibited akt and mapk phosphorylation with ic50 value of 0.015 μm and <0.0063 μm, respectively [1].
target
HER2
References
[1]. nakayama, a., et al., antitumor activity of tak-285, an investigational, non-pgp substrate her2/egfr kinase inhibitor, in cultured tumor cells, mouse and rat xenograft tumors, and in an her2-positive brain metastasis model. j cancer, 2013. 4(7): p. 557-65.
[2]. lyakhov, i., et al., her2- and egfr-specific affiprobes: novel recombinant optical probes for cell imaging. chembiochem, 2010. 11(3): p. 345-50.
[3]. takagi, s., et al., her2 and her3 cooperatively regulate cancer cell growth and determine sensitivity to the novel investigational egfr/her2 kinase inhibitor tak-285. oncoscience, 2014. 1(3): p. 196-204.
TAK-285 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 27996 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 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 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 58 |