Theliatinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Theliatinib 是一种有效且高选择性的 EGFR 抑制剂，具有抗肿瘤活性。野生型 EGFR 的 Ki 为 0.05 nM，EGFR 和 EGFR T790M/L858R 突变体的 IC50 分别为 3 和 22 nM。

Theliatinib a potent and highly selective EGFR inhibitor with anti-tumor activity. Ki of 0.05 nM for wild type EGFR and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant respectively.(In Vivo):Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of 75% at the end of study, and with a dose response.

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Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of75% at the end of study, and with a dose response. Animal Model:NOD-SCID mice injected with esophageal cancer cells (PDECX 1T0950 model)Dosage:2 mg/kg, 5 mg/kg, 15 mg/kg Administration:Oral administration;daily; for 21 days Result:Attenuated tumor growth in PDECX 1T0950 model in a dose-dependent manner.

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Angiogenesis

EGFR

EGFR

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1353644-70-8

442.5

C25H26N6O2

>98% (HPLC)

DMSO:47 mg/mL (106.21 mM)

[H][C@]12CCN(C)[C@@]1([H])CN(C2)C(=O)Nc1cc2c(Nc3cccc(c3)C#C)ncnc2cc1OC

(3aR6aR)-N-(4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)-1-methylhexahydropyrrolo[34-b]pyrrole-5(1H)-carboxamide

(-20℃)

With Ice Pack

≥ 2 years