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CO-1686

Chemical Structure : CO-1686

CAS No.: 1374640-70-6

CO-1686 (Rociletinib;AVL-301;CNX-419)

Catalog No.: PC-44666Not For Human Use, Lab Use Only.

Rociletinib (CO1686, AVL-301, CNX-419) is a potent, highly selective, irreversible inhibitor of mutant EGFR with Ki of 21.5 nM for EGFR L858R/T790M.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Rociletinib (CO1686, AVL-301, CNX-419) is a potent, highly selective, irreversible inhibitor of mutant EGFR with Ki of 21.5 nM for EGFR L858R/T790M.
Rociletinib shows 22-fold selective over WT EGFR; EGFR del19, T790M, L858R/T790M and L858R mutant kinases demonstrates the highest degree of inhibition at 0.1 uM; orally bioavailable.

Physicochemical Properties

M.Wt 555.5515
Formula C27H28F3N7O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 43 mg/mL

Chemical Name/SMILES

2-Propenamide, N-[3-[[2-[[4-(4-acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-

References

1. Walter AO, et al. Cancer Discov. 2013 Dec;3(12):1404-15.

2. Tjin Tham Sjin R, et al. Mol Cancer Ther. 2014 Jun;13(6):1468-79.

3. Sequist LV, et al. N Engl J Med. 2015 Apr 30;372(18):1700-9.

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