CO-1686 hydrobromide
CAS No. 1446700-26-0
CO-1686 hydrobromide( Rociletinib hydrobromide | AVL-301 hydrobromide | CNX-419 hydrobromide )
Catalog No. M11900 CAS No. 1446700-26-0
A potent, highly selective, irreversible inhibitor of mutant EGFR with Ki of 21.5 nM for EGFR L858R/T790M.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
50MG | 147 | Get Quote |
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100MG | Get Quote | Get Quote |
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200MG | Get Quote | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameCO-1686 hydrobromide
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, highly selective, irreversible inhibitor of mutant EGFR with Ki of 21.5 nM for EGFR L858R/T790M.
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DescriptionA potent, highly selective, irreversible inhibitor of mutant EGFR with Ki of 21.5 nM for EGFR L858R/T790M; 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.Breast Cancer Phase 2 Clinical.
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In VitroRociletinib (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.
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In VivoRociletinib (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice.
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SynonymsRociletinib hydrobromide | AVL-301 hydrobromide | CNX-419 hydrobromide
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PathwayAngiogenesis
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TargetEGFR
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RecptorEGFR
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Research AreaCancer
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IndicationBreast Cancer
Chemical Information
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CAS Number1446700-26-0
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Formula Weight636.4634
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Molecular FormulaC27H29BrF3N7O3
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 59 mg/mL
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SMILESCC(=O)N1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F)OC.Br
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Chemical Name2-Propenamide, N-[3-[[2-[[4-(4-acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-, hydrobromide (1:1)
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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.
molnova catalog
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