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Olafertinib (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $41 | In Stock | |
5 mg | $97 | In Stock | |
10 mg | $155 | In Stock | |
25 mg | $322 | In Stock | |
50 mg | $472 | In Stock | |
100 mg | $693 | In Stock | |
1 mL x 10 mM (in DMSO) | $113 | In Stock |
Description | Olafertinib (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC. |
Targets&IC50 | EGFR (WT):689 nM (GI50), EGFR (L858R/T790M):5 nM (GI50), EGFR (del19):10 nM (GI50) |
In vitro | CK-101 specifically targets the mutant forms of EGFR, including T790M, while exhibiting minimal activity toward WT EGFR. It selectively inhibits cell proliferation of cell lines expressing both the activating (HCC827, IC50 <15 nM) and resistance mutations (NCI-H1975, IC50 <5 nM). |
In vivo | CK-101 significantly inhibits tumor growth in EGFR-mutated NSCLC tumor xenograft models, with no activity in the WT EGFR tumor xenograft model. |
Alias | RX-518, EGFR-IN-3, CK-101 |
Molecular Weight | 530.57 |
Formula | C29H28F2N6O2 |
Cas No. | 1660963-42-7 |
Smiles | OCCN1CCN(CC1)c1ccc(Nc2ncc3cccc(-c4cccc(NC(=O)C=C)c4)c3n2)c(F)c1F |
Relative Density. | 1.350 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: Insoluble DMSO: 120 mg/mL (226.18 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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