CO1686 free base · Synonyms: CO-1686 | AVL-301 | CNX-419

Rociletinib is an orally delivered kinase inhibitor.

For research use only. Not for human or veterinary use.

Target EGFR

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

CO1686 structure

CAS No.: 1374640-70-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
2 g	USD 360.00	BP-02467-2g	In stock	Get quote
3 g	USD 440.00	BP-02467-3g	In stock	Get quote
5 g	USD 580.00	BP-02467-5g	In stock	Get quote
10 g	USD 942.00	BP-02467-10g	In stock	Get quote

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Description

Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

Biological activity

In Vitro Rociletinib (CO-1686) (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition. In Vivo Rociletinib (CO-1686) (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (CO-1686) (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice.

Identifiers

SMILES: COC1=CC(=CC=C1NC1=NC=C(C(NC2=CC=CC(NC(=O)C=C)=C2)=N1)C(F)(F)F)N1CCN(CC1)C(C)=O
InChIKey: HUFOZJXAKZVRNJ-UHFFFAOYSA-N

Specifications

MW (average): 555.5515
Formula: C₂₇H₂₈F₃N₇O₃
CAS No.: 1374640-70-6
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO

Documents

References

[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.

Same target

Search EGFR

Same research area

Search Cancer