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Olmutinib
CAS No. 1802181-20-9
Olmutinib( BI1482694,HM61713 )
Catalog No. M21951 CAS No. 1802181-20-9
Olmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase InhibitorOlmutinib at 3 μM significantly reversed drug resistance mediated by ABCG2, but not by ABCB1 and ABCC1, by antagonizing the drug efflux function in ABCG2-overexpressing cells.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
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Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 27 | In Stock |
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| 5MG | 47 | In Stock |
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| 10MG | 77 | In Stock |
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| 25MG | 120 | In Stock |
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| 50MG | 176 | In Stock |
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| 100MG | 267 | In Stock |
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| 200MG | 439 | In Stock |
|
| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameOlmutinib
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NoteResearch use only, not for human use.
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Brief DescriptionOlmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase InhibitorOlmutinib at 3 μM significantly reversed drug resistance mediated by ABCG2, but not by ABCB1 and ABCC1, by antagonizing the drug efflux function in ABCG2-overexpressing cells.
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DescriptionOlmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase InhibitorOlmutinib at 3 μM significantly reversed drug resistance mediated by ABCG2, but not by ABCB1 and ABCC1, by antagonizing the drug efflux function in ABCG2-overexpressing cells. In addition, olmutinib at reversal concentration affected neither the protein expression level nor the localization of ABCG2. The results observed from the accumulation/efflux study of olmutinib showed that olmutinib reversed ABCG2-mediated MDR with an increasing intracellular drug accumulation due to inhibited drug efflux. We also had consistent results with the ATPase assay that olmutinib stimulated ATPase activity of ABCG2 up to 3.5-fold. Additionally, the molecular interaction between olmutinib and ABCG2 was identified by docking simulation. Olmutinib not only interacts directly with ABCG2 but also works as a competitive inhibitor of the transport protein.
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In Vitro——
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In Vivo——
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SynonymsBI1482694,HM61713
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PathwayAngiogenesis
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TargetEGFR
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RecptorEGFR
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Research Area——
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Indication——
Chemical Information
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CAS Number1802181-20-9
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Formula Weight486.6
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Molecular FormulaC26H26N6O2S?
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Purity>98% (HPLC)
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Solubility——
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SMILESCN1CCN(CC1)c1ccc(cc1)Nc1nc2c(c(n1)Oc1cccc(c1)NC(=O)C=C)scc2
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Chemical Name——
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. Zhang W , Fan Y F , Cai C Y , et al. Olmutinib (BI1482694/HM61713), a Novel Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, Reverses ABCG2-Mediated Multidrug Resistance in Cancer Cells[J]. Frontiers in Pharmacology, 2018, 9.2. Zhang Z , Fu L , Guo X , et al. Olmutinib (HM61713) reversed multidrug resistance by inhibiting the activity of ATPbinding cassette subfamily G member 2 in vitro and in vivo[J]. 2018,008(004):563-574.
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