EGFR-IN-1 TFA|西域试剂

EGFR-IN-1 TFA,99.05%

产品编号：Bellancom-19617B| 分子式：C₃₀H₃₁F₃N₆O₆| 分子量：628.60

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货号	价格	库存与货期
Bellancom-19617B	￥4800.00	杭州北京（现货）
Bellancom-19617B	￥8000.00	杭州北京（现货）
Bellancom-19617B	￥17000.00	杭州北京（现货）
Bellancom-19617B	￥28000.00	杭州北京（现货）
Bellancom-19617B	￥43000.00	杭州北京（现货）

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EGFR-IN-1 TFA

产品介绍

EGFR-IN-1 TFA 是一种口服活性不可逆的突变型选择性 L858R/T790M EGFR 抑制剂。与野生型 EGFR 相比，EGFR-IN-1 TFA 对 Gefitinib 耐药的 EGFR L858R/T790M 有 100 倍的抑制作用。EGFR-IN-1 TFA 对 H1975 细胞和 HCC827 细胞具有较强的抗增殖活性。具有抗肿瘤活性。

生物活性

EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.

体外研究

EGFR-IN-1 TFA (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	NSCLC cell lines H1975 (T790M/L858R), HCC827 (∆746-750)
Concentration:	10 μM
Incubation Time:	72 hours
Result:	Inhibited H1975 nonsmall cell lung cancer cell line and the first line mutant HCC827 cell line with IC50s of 4 and 28 nM, respectively.

体内研究
(In Vivo)

EGFR-IN-1 TFA (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight.
EGFR-IN-1 TFA evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 TFA shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 TFA reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (397.71 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5908 mL	7.9542 mL	15.9084 mL
5 mM	0.3182 mL	1.5908 mL	3.1817 mL
10 mM	0.1591 mL	0.7954 mL	1.5908 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献