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Senexin B
CAS No. 1449228-40-3
Senexin B( SNX2-1-165 )
Catalog No. M11929 CAS No. 1449228-40-3
Senexin B (SNX2-1-165) is a highly potent, selective and orally available CDK8/CDK19 inhibitor with IC50 of 24-50 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 248 | In Stock |
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| 10MG | 372 | In Stock |
|
| 25MG | 620 | In Stock |
|
| 50MG | 881 | In Stock |
|
| 100MG | 1188 | In Stock |
|
| 200MG | Get Quote | In Stock |
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| 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 NameSenexin B
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NoteResearch use only, not for human use.
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Brief DescriptionSenexin B (SNX2-1-165) is a highly potent, selective and orally available CDK8/CDK19 inhibitor with IC50 of 24-50 nM.
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DescriptionSenexin B (SNX2-1-165) is a highly potent, selective and orally available CDK8/CDK19 inhibitor with IC50 of 24-50 nM; exhibits selectivity for CDK8 and CDK19 with Kd of 140 nM and 80 nM, respectively; significantly suppresses tumor growth in ER-positive breast cancer xenografts.
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In VitroSenexin B inhibits CDK8/19 in low nanomolar range. Senexin B is a newly optimized derivative of Senexin A. It has the same high selectivity for CDK8/19 and is more potent than Senexin A. Senexin B strongly reduces the emergence of estrogen independent cells. Senexin B shows synergy with fulvestrant in MCF7, T47D-ER/Luc and BT474.
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In VivoPretreatment of tumor-free mice with Senexin B significantly inhibits the growth of triple-negative breast cancer (TNBC) cells inoculated into mice subsequently to Senexin B administration, indicating a general chemopreventive effect on the normal tissue “soil”. Senexin B potentiates the tumor-suppressive effect of doxorubicin on established TNBC xenografts; this effect is associated with the suppression of NFκB-mediated transcriptional induction of tumor-promoting cytokines. Senexin B inhibits invasive growth into the muscle layer in an orthotopic xenograft model of MDA-MB-468 TNBC cells. In a spleen-to-liver colon cancer metastasis model of syngeneic mouse CT26 tumors, Senexin B treatment of mice have the same effect as CDK8 knockdown in tumor cells: suppression of metastatic growth in the liver without a significant effect on primary tumor growth in the spleen. Senexin B suppresses tumor growth and augmentes the effects of fulvestrant in ER-positive breast cancer xenografts.
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SynonymsSNX2-1-165
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PathwayAngiogenesis
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TargetCDK
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RecptorCDK
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Research Area——
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Indication——
Chemical Information
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CAS Number1449228-40-3
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Formula Weight450.53
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Molecular FormulaC27H26N6O
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESO=C(C1=CC2=CC=C(CCNC3=C4C(C=CC(C#N)=C4)=NC=N3)C=C2C=C1)N5CCN(C)CC5
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Chemical Name4-((2-(6-(4-Methylpiperazine-1-carbonyl)naphthalen-2-yl)ethyl)amino)quinazoline-6-carbonitrile
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. Donald C. Porter, et al. Abstract PR08: Targeting tumor microenvironment with selective small-molecule inhibitors of CDK8/19.
2. Cdk8/cdk19 selective inhibitors and their use in anti-metastatic and chemopreventative methods for cancer. Publication number: WO2013116786 A1.
3. McDermott MS, et al. Oncotarget. 2017 Feb 21;8(8):12558-12575.
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