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Rociletinib

Catalog No. T2369 CAS 1374640-70-6

Synonyms: AVL-301, CNX-419, CO-1686

Rociletinib (CNX-419) is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity.

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Rociletinib, CAS 1374640-70-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 45.00
10 mg	In stock	$ 68.00
25 mg	In stock	$ 100.00
50 mg	In stock	$ 126.00
100 mg	In stock	$ 207.00
1 mL * 10 mM (in DMSO)	In stock	$ 53.00

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Purity: 99.25%

Purity: 98.75%

Purity: 98.39%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Rociletinib (CNX-419) is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity.
Targets&IC50	EGFR (WT):303.3 nM(Ki), EGFR (L858R/T790M):21.5 nM(Ki)
In vitro	CO-1686 demonstrates significant dose-dependent tumor growth inhibition across all models of EGFR mutations, including transgenic mice expressing EGFRL858R- and EGFRL858R/T790M.
In vivo	CO-1686 selectively inhibits the growth of NSCLC (non-small cell lung cancer) cells expressing mutant EGFR, with a GI50 range of 7 to 32 nM, and induces apoptosis. NSCLC cell lines resistant to CO-1686 show signs of epithelial-mesenchymal transition and increased sensitivity to AKT inhibitors. In cells expressing mutant EGFR, CO-1686 inhibits p-EGFR with an IC50 range of 62 to 187 nM, while also inhibiting EGFR phosphorylation in three types of cells expressing WT (wild type) EGFR, with an IC50 of >2,000 nM.
Kinase Assay	Inhibition Kinetics Studies: Recombinant human wild-type and T790M/L858R double mutant EGFR, both Nterminal GST-tagged, are used in the assay. The Omnia continuous read assay is performed as described by the vendor.
Cell Research	Cells are seeded at 3,000 cells per well in growth media supplemented with 5% FBS, 2 mmol/L, L-glutamine, and 1% penicillin–streptomycin, allowed to adhere overnight, and treated with a dilution series of test compounds for 72 hours. Cell viability is determined by CellTiter-Glo, and results are represented as background-subtracted relative light units normalized to a dimethyl sulfoxide (DMSO)–treated control. Growth inhibition (GI 50) values are determined by GraphPad Prism 5.04. MK-2206 and XL-880 compounds are obtained from Selleck Chemical. CI data are generated using CalcuSyn.(Only for Reference)

Synonyms	AVL-301, CNX-419, CO-1686
Molecular Weight	555.55
Formula	C27H28F3N7O3
CAS No.	1374640-70-6

Storage

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

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (167.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Walter AO, et al. Cancer Discov. 2013. doi:10.1158/2159-8290.CD-13-0314

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Drug Library Highly Selective Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Approved Drug Library FDA-Approved & Pharmacopeia Drug Library NO PAINS Compound Library Apoptosis Compound 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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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 1374640-70-6 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR CNX 419 AVL 301 HER1 Inhibitor inhibit AVL-301 CO 1686 CNX-419 ErbB-1 AVL301 CO-1686 CNX419 Epidermal growth factor receptor CO1686 inhibitor

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