| Identification | Back Directory | [Name]
(3aR,6aR)-N-(4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)-1-methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxamide | [CAS]
1353644-70-8 | [Synonyms]
HMPL309
HMPL-309
HMPL 309
EOS-61583
Theliatinib
Theliatinib (HMPL-309)
ThTheliatinib (HMPL-309)
HMPL-309;HMPL 309;HMPL309
(3aR,6aR)-N-(4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)-1-methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxamide | [Molecular Formula]
C25H26N6O2 | [MDL Number]
MFCD32173988 | [MOL File]
1353644-70-8.mol | [Molecular Weight]
442.51 |
| Chemical Properties | Back Directory | [Boiling point ]
675.6±55.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 5 mg/mL (11.30 mM) | [form ]
Solid | [pka]
13.59±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
Theliatinib (HMPL-309) is a potent EGFR inhibitor with a Ki value of 0.05 nM for EGFR and IC50 values of 3 nM and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively. It is more than 50-fold selective for EGFR over 72 other kinases. | [in vitro]
Compared with erlotinib or gefitnib, theliatinib has stronger binding affinity to wild-type EGFR and is more difficult to be replaced by ATP, which makes theliatinib have better target binding effect, and the EGFR-activated tumors have stronger antitumor activity. | [in vivo]
Theliatinib has concentration-dependent antitumor activity in a series of patient-derived esophageal cancer xenograft models. But aberrant activation or genetic mutation of other targets such as PI3K and FGFR attenuates the antitumor activity of EGFR inhibitors, especially theliatinib. | [target]
| Target | Value | WT EGFR
(Cell-free assay) | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> 3 nM EGFR T790M/L858R
(Cell-free assay) | 22 nM |
| [storage]
Store at -20°C |
|
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|