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Olafertinib

🥰Excellent
Catalog No. TQ0255Cas No. 1660963-42-7
Alias RX-518, EGFR-IN-3, CK-101

Olafertinib (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC.

Olafertinib

Olafertinib

🥰Excellent
Purity: 98.43%
Catalog No. TQ0255Alias RX-518, EGFR-IN-3, CK-101Cas No. 1660963-42-7
Olafertinib (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC.
Pack SizePriceAvailabilityQuantity
1 mg38 €In Stock
5 mg92 €In Stock
10 mg147 €In Stock
25 mg305 €In Stock
50 mg448 €In Stock
100 mg658 €In Stock
1 mL x 10 mM (in DMSO)107 €In Stock
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Purity:98.43%
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Product Introduction

Bioactivity
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.
AliasRX-518, EGFR-IN-3, CK-101
Chemical Properties
Molecular Weight530.57
FormulaC29H28F2N6O2
Cas No.1660963-42-7
SmilesOCCN1CCN(CC1)c1ccc(Nc2ncc3cccc(-c4cccc(NC(=O)C=C)c4)c3n2)c(F)c1F
Relative Density.1.350 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.8848 mL9.4238 mL18.8477 mL94.2383 mL
5 mM0.3770 mL1.8848 mL3.7695 mL18.8477 mL
10 mM0.1885 mL0.9424 mL1.8848 mL9.4238 mL
20 mM0.0942 mL0.4712 mL0.9424 mL4.7119 mL
50 mM0.0377 mL0.1885 mL0.3770 mL1.8848 mL
100 mM0.0188 mL0.0942 mL0.1885 mL0.9424 mL

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