| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Rociletinib hydrobromide (CO-1686; AVL-301; CNX-419), the hydrobromide salt of Rociletinib, is an oral, irreversible/covalent, and mutant-selective EGFR inhibitor (EGFR-TKI) with antitumor activity. It inhibits EGFRL858R/T790M and EGFRWT with Ki values of 21.5 nM and 303.3 nM in cell-free assays, respectively. Rociletinib binds to and inhibits mutant forms of EGFR, including T790M, thereby leading to cell death of resistant tumor cells. Compared to other EGFR inhibitors, Rociletinib inhibits T790M, a secondary acquired resistance mutation, as well as other mutant EGFRs and may have therapeutic benefits in tumors with T790M-mediated resistance to other EGFR tyrosine kinase inhibitors.
| ln Vitro |
Rociletinib (0.1 μM) potently and irreversibly inhibits EGFR and inhibits more than 50% of 23 targets. Rociletinib potently and specifically inhibits the proliferation and promotes death of NSCLC cells expressing mutant EGFR. Rociletinib-resistant NSCLC cell lines are responsive to AKT inhibition [1].
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| ln Vivo |
An NSCLC xenograft model with an EGFR mutation shows antitumor efficacy when treated with rociletinib (100 mg/kg/day, orally). The anticancer efficacy of rociletinib (50 mg/kg bid, po) has been shown in transgenic mice that express human EGFR-L858R and EGFR-L858R-T790M [1].
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| 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
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| Molecular Formula |
C₂₇H₂₉BRF₃N₇O₃
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|---|---|
| Molecular Weight |
636.46
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| CAS # |
1446700-26-0
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| Related CAS # |
Rociletinib;1374640-70-6
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| SMILES |
C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C(C)=O)CC4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O.[H]Br
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| Synonyms |
CO-1686 hydrobromide AVL-301 hydrobromide CNX-419 hydrobromideCO1686AVL-301 CNX419CO-1686 AVL 301 CNX 419CO 1686 AVL301 CNX-419.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 59 mg/mL (~92.70 mM)
H2O : < 0.1 mg/mL |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5712 mL | 7.8560 mL | 15.7119 mL | |
| 5 mM | 0.3142 mL | 1.5712 mL | 3.1424 mL | |
| 10 mM | 0.1571 mL | 0.7856 mL | 1.5712 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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