EGF816
- CAS NO.:1508250-71-2
- Empirical Formula: C26H31ClN6O2
- Molecular Weight: 495.02
- MDL number: MFCD28963918
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-01 18:44:47
What is EGF816?
Description
Nazartinib is an irreversible inhibitor of mutant EGF receptors (EGFRs). It is selective for EGFR mutant cell lines, including H3255 and HCC827 lung adenocarcinoma cells (IC50s = 6.11 and 1.52 nM, respectively) and resistant H1975 non-small cell lung cancer cells (NSCLC; IC50 = 4.18 nM), over cells expressing wild-type EGFRs (IC50 = 160.6 nM for HaCaT keratinocytes). Nazartinib decreases phosphorylation of EGFR in H3255, HCC827, and H1975 cells (EC50s = 5, 1, and 3 nM, respectively) and inhibits cell proliferation (EC50s = 9, 11, and 25 nM, respectively) but does not affect cell proliferation in cell lines containing wild-type EGFR. It reduces tumor growth in an HCC827 lung adenocarcinoma mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg per day for 21 days.
in vitro
egf816 showed sustained inhibition of pegfr, which is consistent with the irreversible binding mechanism of egf816. egf816 also performs exceptionally well in long term dosing studies providing durable responses in the preclinical models [1].
in vivo
egf816 demonstrated strong in vivo tumor regressions in several egfr activating and resistant tumor models. in all of the models egf816 inhibited tumor growth dose-dependently and achieved regressions of established tumors at well tolerated doses [1].
References
[1] shailaja kasibhatla, jie li, celin tompkins, mei-ting vaillancourt, jennifer anderson, annemarie culazzo pferdekamper, chun li, oliver long, mathew mcneill, robert epple, debbie liao, eric murphy, steve bender, yong jia, gerald lelais. egf816, a novel covalent inhibitor of mutant-selective epidermal growth factor receptor, overcomes t790m-mediated resistance in nsclc. [abstract]. in: proceedings of the 105th annual meeting of the american association for cancer research; 2014 apr 5-9; san diego, ca. philadelphia (pa): aacr; cancer res 2014;74(19 suppl):abstract nr 1733. doi:10.1158/1538-7445.am2014-1733
Properties of EGF816
Density | 1.28±0.1 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | Soluble in DMSO |
form | Powder |
pka | 11.38±0.43(Predicted) |
color | Off-white to yellow |
Safety information for EGF816
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for EGF816
Related products of tetrahydrofuran
You may like
-
Egf816 95% CAS 1508250-71-2View Details
1508250-71-2 -
ZIRCONIUM AAS SOLUTION 99%View Details
-
FUCHSIN BASIC 0.1% SOLUTION 99%View Details
-
1 10-PHENANTHROLIN HYDROCHLORIDE 99%View Details
-
ERDMANS REAGENT (FOR PROTEIN TEST) 99%View Details
-
OXALIC ACID SOLUTION 0.1 N 99%View Details
-
ALKALINE COPPER SOLUTION 99%View Details
-
A-AMYLASE (DIASTASE) 99%View Details