EGFR-IN-1 TFA

立即咨询

EGFR-IN-1 TFA

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

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 irreversibleL858R/T790M mutant selectiveEGFRinhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistantEGFRL858R, T790M with 100-fold selectivity over wild-typeEGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity^[1].

IC₅₀& Target^[1]

EGFR^L858R/T790M

体外研究
(In Vitro)

EGFR-IN-1 TFA (compound 24) is an orally active and irreversibleL858R/T790M mutant selective EGFRinhibitor. 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^[1].

Cell Proliferation Assay^[1]

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^[1].
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^[1].

分子量

628.60

性状

Solid

Formula

C₃₀H₃₁F₃N₆O₆

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)

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。