Senexin B

SKU: orb1941081

Description

Senexin 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.

Key Properties

• CAS Number: 1449228-40-3
• MW: 450.53
• Purity: >98% (HPLC)
• Formula: C₂₇H₂₆N₆O
• SMILES: O=C(C1=CC2=CC=C(CCNC3=C4C(C=CC(C#N)=C4)=NC=N3)C=C2C=C1)N5CCN(C)CC5
• Target: CDK
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Pretreatment 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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• In Vitro:
  Senexin 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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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SNX2-1-165

Quick Database Links

Gene Symbol

CDK