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Rociletinib hydrobromide

Catalog No. T14993 CAS 1446700-26-0

Synonyms: AVL-301 hydrobromide, CO-1686 (hydrobromide), CNX-419 hydrobromide

Rociletinib hydrobromide is an orally delivered inhibitor of the mutant form of EGFR kinase (Kis: 21.5 nM and 303.3 nM for EGFR L858R/T790M and EGFR WT).

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Rociletinib hydrobromide Chemical Structure

Rociletinib hydrobromide, CAS 1446700-26-0

Pack Size	Availability	Price/USD
5 mg	5 days	$ 39.00
10 mg	5 days	$ 67.00
1 mL * 10 mM (in DMSO)	5 days	$ 55.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Rociletinib hydrobromide is an orally delivered inhibitor of the mutant form of EGFR kinase (Kis: 21.5 nM and 303.3 nM for EGFR L858R/T790M and EGFR WT).
Targets&IC50	EGFR (T790M):303.3 nM （ki）, EGFR (L858R/T790M):21.5 nM （ki）
In vitro	Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition. Rociletinib selectively inhibits the growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib (0.1 μM) inhibits EGFR potently and irreversibly. It inhibits more than 50% of 23 targets.
In vivo	Rociletinib (50 mg/kg bid, p.o.) shows anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice. Rociletinib (100 mg/kg/day, p.o.) displays anti-tumor activity in NSCLC EGFR mutant xenograft models.

Synonyms	AVL-301 hydrobromide, CO-1686 (hydrobromide), CNX-419 hydrobromide
Molecular Weight	636.46
Formula	C27H29BrF3N7O3
CAS No.	1446700-26-0

Storage

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

Solubility Information

DMSO: 59 mg/mL (92.70 mM)

References and Literature

1. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25.

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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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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

Rociletinib hydrobromide 1446700-26-0 Others AVL-301 Hydrobromide AVL-301 hydrobromide CNX 419 Hydrobromide CO 1686 AVL301 Hydrobromide CO-1686 (hydrobromide) CO-1686 CNX-419 Hydrobromide Rociletinib Hydrobromide CO1686 CNX419 Hydrobromide CNX-419 hydrobromide AVL 301 Hydrobromide inhibitor inhibit

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