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EGFR-IN-2 Sale

目录号 : GC33195

EGFR-IN-2是一种非共价的,不可逆的,突变选择性的二代EGFR抑制剂。

EGFR-IN-2 Chemical Structure

Cas No.:1643497-70-4

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Animal experiment:

Mice[1]Eight week old female SCID beige mice are inoculated subcutaneously with 5×106 NCI-H1975 cells. When tumors reach a mean volume of 300 to 500 mm3, mice with similarly sized tumors are randomized into treatment groups. EGFR-IN-2 at 50 mg/kg or 100 mg/kg is administered orally as a single dose. Tumor and plasma samples are collected at 2, 8 or 16 h post dose[1].

References:

[1]. Chan BK, et al. Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor. J Med Chem. 2016 Oct 13;59(19):9080-9093.

产品描述

EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.

EGFR-IN-2 (Compound 21) inhibits EGFR autophosphorylation with IC50s of 0.027 μM, 0.009 μM ,0.033 μM , and 0.218 μM in double mutant TMLR cell line H1975, double mutant TMdel cell line PC9-ER, activating mutant del70% when tested at 0.1 μM, 61-fold over the TMLR Ki and 63-fold over the TMdel Ki)[1].

To examine its inhibitory effect on pEGFR levels in vivo, EGFR-IN-2 (Compound 21) is studied in a mouse H1975 (TMLR) xenograft model. After a single oral dose of 21 at 50 mg/kg, free plasma concentrations of EGFR-IN-2 at or exceeding the in vitro p-EGFR IC50 of 0.027 μM are sustained over 8 h. When administered at 100 mg/kg, the coverage of p-EGFR IC50 is extended to the last measured time point of 16 h postdose. Corresponding knockdown of p-EGFR and the downstream effectors pERK1/2 and AKT levels are observed at those time points, suggesting target engagement in vivo. In mouse, after intravenous and oral administration, the plasma clearance of EGFR-IN-2 is determined to be 104 mL/kg per min with a bioavailability of 19%. In dogs, the plasma clearance is 13 mL/kg per min with an oral bioavailability of 30%[1].

[1]. Chan BK, et al. Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor. J Med Chem. 2016 Oct 13;59(19):9080-9093.

Chemical Properties

Cas No. 1643497-70-4 SDF
Canonical SMILES O=S(N(N=C1)C=C1C2=NC=CC(NC3=NC=C(C(N4CC(C(C)(O)C)C4)=NN5[C@H](CC)C)C5=C3)=N2)(C6CC6)=O
分子式 C26H33N9O3S 分子量 551.66
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.8127 mL 9.0636 mL 18.1271 mL
5 mM 0.3625 mL 1.8127 mL 3.6254 mL
10 mM 0.1813 mL 0.9064 mL 1.8127 mL
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