货号	规格	价格	上海	北京	珠海	重庆	武汉
S88457-5mg	≥98%	￥3050.00 S88457-5mg ￥3050.00 3-5天	0 货期：3-5天	-	-	-	-
S88457-10mg	≥98%	￥4370.00 S88457-10mg ￥4370.00 3-5天	0 货期：3-5天	-	-	-	-
S88457-25mg	≥98%	￥6970.00 S88457-25mg ￥6970.00 3-5天	0 货期：3-5天	-	-	-	-
S88457-50mg	≥98%	￥9390.00 S88457-50mg ￥9390.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.

靶点：

EGFR/HER2;EGFR; HER

体内研究：

A prototypic WT EGFR driven xenograft model (A431) is used to benchmark Tarloxotinib bromide activity against each EGFR-TKI by “retrotranslation” of reported plasma exposure for each agent in human subjects back to the xenograft model. Only treatment with clinically relevant doses and schedules of Tarloxotinib bromide is associated with tumor regression and durable inhibition of WT EGFR tumor phosphorylation. Consistent with these findings, Tarloxotinib bromide treatment can also regress the WT EGFR NSCLC tumor models H125 and H1648, demonstrating Tarloxotinib bromide provides the necessary therapeutic index to inhibit WT EGFR in vivo

参考文献：

1. Shevan Silva, Abstract A67: Preclinical efficacy of tarloxotinib bromide (TH-4000), a hypoxia-activated EGFR/HER2 inhibitor: rationale for clinical evaluation in EGFR mutant, T790M-negative NSCLC following progression on EGFR-TKI therapy. Abstracts: AACR- 2. Adam V. Patterson, Abstract 5358: The hypoxia-activated EGFR-TKI TH-4000 overcomes erlotinib-resistance in preclinical NSCLC models at plasma levels achieved in a Phase 1 clinical trial. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.467 ml	7.334 ml	14.668 ml
5 mM	0.293 ml	1.467 ml	2.934 ml
10 mM	0.147 ml	0.733 ml	1.467 ml
50 mM	0.029 ml	0.147 ml	0.293 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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