CAS No. 1508250-71-2
| IUPAC Name | N-[7-chloro-1-[(3R)-1-[(E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]benzimidazol-2-yl]-2-methylpyridine-4-carboxamide | |
|---|---|---|
| CAS Number | 1508250-71-2 | |
| Molecular Formula |
C26H31ClN6O2 |
|
| Molecular Weight (MW) | 495.02 | |
| SMILES | CC1=NC=CC(=C1)C(=O)NC2=NC3=C(N2C4CCCCN(C4)C(=O)C=CCN(C)C)C(=CC=C3)Cl | |
| InChIKey | IOMMMLWIABWRKL-WUTDNEBXSA-N |
Nazartinib (EGF816) is a covalent, irreversible, mutant-selective epidermal growth factor receptor (EGFR) inhibitor with nanomolar inhibitory potency against EGFR activating mutations (L858R, ex19del) and the T790M resistance mutation, demonstrating up to 60-fold selectivity over wild-type EGFR in vitro. Inhibition of mutant EGFR suppresses downstream receptor autophosphorylation and oncogenic signaling pathways, leading to the inhibition of cell proliferation and regression of tumor growth in EGFR-mutant non-small cell lung cancer models. [1][2]
|
Concentration
Volume
Mass
|
|---|
| Solvent | Solubility & Note |
|---|---|
| DMSO |
99 mg/mL
(199.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Ethanol | 99 mg/mL |
| Water | Insoluble |
| DMSO |
100 mg/mL
(202.01 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Ethanol | 100 mg/mL |
| Water | Insoluble |
- Preheat media/saline to 37°C.
- Mix rapidly (pipette/vortex) upon addition.
- For complex mixes, always add the aqueous phase last.
- Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).
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- Nazartinib (EGF816) Clinical Trials
- Nazartinib (EGF816) Solubility in DMSO
- Nazartinib (EGF816) Stock Solution
- Nazartinib (EGF816) Storage
- Nazartinib (EGF816) Stability
- Nazartinib (EGF816) Molecular Weight
- Nazartinib (EGF816) SMILES
- Nazartinib (EGF816) Chemical Structure (2D and 3D)
- Nazartinib (EGF816) SDS|MSDS