Structure
Rociletinib hydrobromide, Inhibitor
Rociletinib hydrobromide
Purity
98.00%
Synonyms
Rociletinib hydrobromide; CO-1686 (hydrobromide); AVL-301 hydrobromide; CNX-419 hydrobromide; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 59mg/mL (92.70mM)
H2O: <0.1mg/mL (insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
H2O: <0.1mg/mL (insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C27H29BrF3N7O3
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
CAS Number
1446700-26-0
Target & IC50
EGFRL858R/T790M: ic50 21.5nM (ki)
EGFRT790M: ic50 303.3nM (ki)
EGFRT790M: ic50 303.3nM (ki)
In Vitro
Rociletinib (50mg/kg bid, p.o.) shows anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice. Rociletinib (100mg/kg/day, p.o.) displays anti-tumor activity in NSCLC EGFR mutant xenograft models.
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for Rociletinib hydrobromide, inhibitor
Rociletinib hydrobromide is an orally delivered inhibitor of the mutant form of EGFR kinase (Kis: 21.5nM and 303.3nM for EGFR L858R/T790M and EGFR WT).
References
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.
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.
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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Product Notes
The Rociletinib hydrobromide (Catalog #AAA5754732) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Rociletinib hydrobromide, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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