NVS-816
EGF816
CAS: 1508250-71-2
Molecular Formula: C26H31ClN6O2
NVS-816 - Names and Identifiers
NVS-816 - Physico-chemical Properties
| Molecular Formula | C26H31ClN6O2 |
| Molar Mass | 495.02 |
| Density | 1.28±0.1 g/cm3(Predicted) |
| Solubility | DMSO: ≥ 242 mg/mL |
| pKa | 11.38±0.43(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | EGF816 is a novel, covalent, and selective EGFR inhibitor for mutant EGFR, with equivalent activity for tumorigenic (L858R and ex19del) and T790M tolerance mutations, its selectivity is higher than that of wild type EGFR. EGF816 potently inhibits common EGFR mutants such as L858R, Ex19del and T790M in vitro. Three cell lines: H3255, HCC827 and H1975 (containing L858R, Ex19del and L858R/T790M mutations, respectively) were used to test the cellular activity of EGF816 against the EGFR mutant. Incubation of cells with EGF816 for 3 H resulted in potent inhibition of pEGFR levels in H3255, HCC827 and H1975 cells with EC50 of 5, 1 and 3 nmol/L, respectively. Cell experiments also demonstrated that EGF816 is more selective for mutant EGFR than wild-type egf816. |
| In vivo study | EGF816 is well tolerated in in vivo experiments with favorable physicochemical properties and oral bioavailability in mice. In rodents, EGF816 has a moderate volume of distribution and a low clearance rate (30% and 35% in the liver blood stream of rats and mice, respectively). In dogs, EGF816 has high clearance and high distribution capacity. EGF816 has anti-tumor activity in a mouse model of exon 20 insertion(EGFR). At concentrations higher than the effective dose, EGF816 had little inhibitory effect on wild-type EGFR and was well tolerated. Single drug treatment, EGF816 sustained inhibition of EGFR phosphorylation, and EGFR occurred irreversible binding. EGF816 has a longer half-life in humans than in mice and is currently in clinical Phase I/II trials. |
NVS-816 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.02 ml | 10.101 ml | 20.201 ml |
| 5 mM | 0.404 ml | 2.02 ml | 4.04 ml |
| 10 mM | 0.202 ml | 1.01 ml | 2.02 ml |
| 5 mM | 0.04 ml | 0.202 ml | 0.404 ml |
Last Update：2024-01-02 23:10:35
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Spot supply
Product Name: EGF816 Visit Supplier Webpage Request for quotationCAS: 1508250-71-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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