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Olafertinib

Catalog No. TQ0255 CAS 1660963-42-7

Synonyms: CK-101, EGFR-IN-3, RX-518

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

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Olafertinib, CAS 1660963-42-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 322.00
50 mg	In stock	$ 472.00
100 mg	In stock	$ 693.00
1 mL * 10 mM (in DMSO)	In stock	$ 113.00

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Purity: 98.43%

Biological Description

Chemical Properties

Storage & Solubility Information

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.

Synonyms	CK-101, EGFR-IN-3, RX-518
Molecular Weight	530.57
Formula	C29H28F2N6O2
CAS No.	1660963-42-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 120 mg/mL (226.18 mM), Sonification is recommended.

References and Literature

1. Xiangping Qian, et al. Abstract 2078: CK-101 (RX518), a mutant-selective inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Prostate Cancer Compound Library Clinical Compound Library NO PAINS Compound Library Covalent Inhibitor Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Olafertinib 1660963-42-7 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR RX 518 CK-101 EGFR-IN-3 CK 101 Inhibitor ErbB-1 Epidermal growth factor receptor CK101 RX-518 NSCLC HER1 RX518 inhibit inhibitor

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