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Rociletinib hydrobromide

Catalog No. T14993Cas No. 1446700-26-0

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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Pack Size	Price	Availability
5 mg	$39	7-10 days
10 mg	$67	7-10 days
1 mL x 10 mM (in DMSO)	$55	7-10 days

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Product Introduction

Bioactivity

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).
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.
Alias	AVL-301 hydrobromide, CO-1686 (hydrobromide), CNX-419 hydrobromide

Chemical Properties

Molecular Weight	636.46
Formula	C27H29BrF3N7O3
Cas No.	1446700-26-0

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 59 mg/mL (92.70 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5712 mL	7.8560 mL	15.7119 mL	78.5595 mL
5 mM	0.3142 mL	1.5712 mL	3.1424 mL	15.7119 mL
10 mM	0.1571 mL	0.7856 mL	1.5712 mL	7.8560 mL
20 mM	0.0786 mL	0.3928 mL	0.7856 mL	3.9280 mL
50 mM	0.0314 mL	0.1571 mL	0.3142 mL	1.5712 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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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