產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg
CAS	871026-44-7
別名
化學(xué)名	N-[2-[4-[3-chloro-4-[3-(trifluoromethyl)phenoxy]anilino]pyrrolo[3,2-d]pyrimidin-5-yl]ethyl]-3-hydroxy-3-methylbutanamide
分子式	C26H25ClF3N5O3
分子量	547.96
溶解度	≥ 27.4mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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