| Cas No.: | 1353644-70-8 |
| Synonyms: | HMPL-309,HMPL 309，HMPL309 |
| SMILES: | C1=CC(NC2C3C=C(NC(=O)N4C[C@@]([H])5N(C)CC[C@]5([H])C4)C(OC)=CC3=NC=N2)=CC(C#C)=C1 |
| Formula: | C25H28N6O2 |
| M.Wt: | 444.23 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Theliatinib (HMPL-309) is a potent, ATP-competitive and highly selective EGFR inhibitor, significantly inhibits phosphorylation of EGFR (p-EGFR) and its downstream targets, AKT and ERK (p-AKT and p-ERK), with anti-tumor activity. Theliatinib (HMPL-309) shows a Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively[1]. |
| Target: | IC50: 3 nM (EGFR), 22 nM (EGFR T790M/L858R)[1] Ki: 0.05 nM (EGFR)[1] |
| References: | [1]. Ren Y, et al. Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification. Oncotarget. 2017 Apr 19;8(31):50832-50844. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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