| Identification | Back Directory | [Name]
TAK-285 | [CAS]
871026-44-7 | [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- | [EINECS(EC#)]
1533716-785-6 | [Molecular Formula]
C26H25ClF3N5O3 | [MDL Number]
MFCD22124520 | [MOL File]
871026-44-7.mol | [Molecular Weight]
547.957 |
| Chemical Properties | Back Directory | [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) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [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]. | [in vivo]
TAK-285 (Compound 34e; 50-100 mg/kg; oral administration; twice daily; for 14 days; female BALB/cAJcl mice) treatment exhibits dose-dependent tumor growth inhibition (tumor/control ratio [T/C]): 44% and 11% at 50 and 100 mg/kg, respectively) without significant body weight loss in mice[1]. | Animal Model: | Female BALB/cAJcl mice (7-weeks old) with 4?1ST xenograft models[1] | | Dosage: | 50 mg/kg, 100 mg/kg | | Administration: | Oral administration; twice daily; for 14 days | | Result: | Exhibited dose-dependent tumor growth inhibition. |
| [target]
HER2 | [IC 50]
EGFR: 23 nM (IC50); HER2: 17 nM (IC50) | [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. |
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| Company Name: |
Jia Xing Isenchem Co.,Ltd
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| Tel: |
0573-85285100 18627885956 |
| Website: |
https://www.chemicalbook.com/ShowSupplierProductsList14265/0.htm |
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