Tuxobertinib

产品说明书

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	同义名 :	BDTX-189
	CAS号 :	2414572-47-5
	货号 :	A1365630
	分子式 :	C₂₉H₂₉ClN₆O₄
	纯度 :	99%
	分子量 :	561.03
	MDL号 :	MFCD32878264
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性
靶点	HER2/ErbB2 HER2, Kd:0.76 nM HER2/ErbB2 HER2, Kd:0.76 nM HER2/ErbB2 HER2, Kd:0.76 nM EGFR/ErbB1 EGFR, Kd:0.2 nM
描述	Tuxobertinib (BDTX-189) serves as a powerful, orally administered, selective inhibitor targeting allosteric EGFR and HER2 oncogenic mutations, notably EGFR/HER2 exon 20 insertion mutants. It demonstrates dissociation constants (KDs) of 0.2, 0.76, 13, and 1.2 nM for EGFR, HER2, BLK, and RIPK2, respectively, and exhibits anticancer activity^[1].

实验方案

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.91mL

1.78mL

0.89mL

17.82mL

3.56mL

1.78mL

参考文献
[1]Elizabeth Buck, et al. BDTX-189, a Potent and Selective Inhibitor of Allosteric EGFR and HER2 Oncogenic Mutations.

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靶点

靶点	数值

HER2/ErbB2	HER2, Kd:0.76 nM
HER2/ErbB2	HER2, Kd:0.76 nM
HER2/ErbB2	HER2, Kd:0.76 nM
EGFR/ErbB1	EGFR, Kd:0.2 nM
EGFR/ErbB1	EGFR, Kd:0.2 nM
EGFR/ErbB1	EGFR, Kd:0.2 nM