Osimertinib
Osimertinib
Osimertinib
| Catalog | Description | Size | Price (USD) | Qty |
|---|---|---|---|---|
| GBM-5036-10MG | Osimertinib | 10mg | $105.00 | |
| GBM-5036-50MG | Osimertinib | 50mg | $315.00 |
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Description
Mutant EGFR kinase inhibitor
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Specifications
Bioassays Specification Bio-Activity Mutant EGFR kinase inhibitor Chemical Name N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide Function / Pharmacology A potent, selective, irreversible inhibitor of mutant EFGR tyrosine kinase1. Osimertinib inhibits phosphorylation of EGFR in T790M-mutant cell lines (IC50 <15 nM) but was less potent at inhibition of EGFR phosphorylation in wild-type cells (IC50s in the range of 480 to 1,865 nM). It produces sustained tumor regression in EGFR-mutant tumor xenograft and transgenic rodent models2. Tumor cells develop resistance to osimertinib but combination treatment with an IL-6 antibody reverses resistance to a certain extent3. In clinical use for treatment of non-small cell lung cancer4. CAS# 1421373-65-0 MW 499.6 Molecular Formula C28H33N7O2 Solubility Soluble in DMSO (up to 40 mg/ml) Supplied powder Storage as supplied -20°C Ship temp Ambient References 1. MRV Finlay et al. J. Med. Chem. 2014 57:8249 2. DAE Cross et al. Cancer Discov. 2014 4:1046 3. J Tan et al. Eur, J. Pharm. Sci. 2024 199:106805 4. H Patel et al. Eur. J. Med. Chem. 2017 142:32 Antibody Specification Alternate Names AZD-9291 Protein Specification Purity >98% - Reviews
| Bioassays Specification | |
| Bio-Activity | Mutant EGFR kinase inhibitor |
| Chemical Name | N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide |
| Function / Pharmacology | A potent, selective, irreversible inhibitor of mutant EFGR tyrosine kinase1. Osimertinib inhibits phosphorylation of EGFR in T790M-mutant cell lines (IC50 <15 nM) but was less potent at inhibition of EGFR phosphorylation in wild-type cells (IC50s in the range of 480 to 1,865 nM). It produces sustained tumor regression in EGFR-mutant tumor xenograft and transgenic rodent models2. Tumor cells develop resistance to osimertinib but combination treatment with an IL-6 antibody reverses resistance to a certain extent3. In clinical use for treatment of non-small cell lung cancer4. |
| CAS# | 1421373-65-0 |
| MW | 499.6 |
| Molecular Formula | C28H33N7O2 |
| Solubility | Soluble in DMSO (up to 40 mg/ml) |
| Supplied | powder |
| Storage as supplied | -20°C |
| Ship temp | Ambient |
| References | 1. MRV Finlay et al. J. Med. Chem. 2014 57:8249 2. DAE Cross et al. Cancer Discov. 2014 4:1046 3. J Tan et al. Eur, J. Pharm. Sci. 2024 199:106805 4. H Patel et al. Eur. J. Med. Chem. 2017 142:32 |
| Antibody Specification | |
| Alternate Names | AZD-9291 |
| Protein Specification | |
| Purity | >98% |