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Senexin B
CDK8/CDK19 inhibitor, highly potent, selective and orally available

Senexin B

Catalog No. A8732
Size Price Stock Qty
5mg $350.00 In stock
25mg $1,200.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

OTX-015

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Chemical Properties

Cas No. 1449228-40-3 SDF Download SDF
Chemical Name 4-((2-(6-(4-methylpiperazine-1-carbonyl)naphthalen-2-yl)ethyl)amino)quinazoline-6-carbonitrile
Canonical SMILES CN(CC1)CCN1C(C2=CC3=CC=C(C=C3C=C2)CCNC4=C(C=C(C#N)C=C5)C5=NC=N4)=O
Formula C27H26N6O M.Wt 450.53
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Senexin B is a highly potent, selective and orally available CDK8/CDK19 inhibitor with IC50 values ranging from 24-50 nM [1].

Cyclin-dependent kinase 8 (CDK8), along with its closely related isoform CDK19, is an oncogenic transcription-regulating kinase. CDK8 plays an essential role in the pluripotent stem cell phenotype. Also, CDK8 is a regulator of several transcriptional programs involved in carcinogenesis and has been identified as an oncogene in melanoma and colon cancer [1].

Senexin B is a highly potent, selective and orally available CDK8/CDK19 inhibitor. Senexin B exhibited selectivity for CDK8 and CDK19 with Kd values of 140 nM and 80 nM. Senexin B was fully soluble in 20% propylene glycol at 1 mM, and fully soluble in water at 50 mM concentration. Senexin B inhibited CDK8/19 in low nanomolar range in vitro and in vivo in an ATP competitive manner [2]. In HT1080 cells, Senexin B inhibited CMV-GFP expression induced by IPTG-inducible p21 [1].

In CB-17 SCID mice (8 weeks old), i.p. injections of Senexin B (40 mg/kg) or carrier for 5 days, mice were then injected s.c. with 1 x 106 cells of human A549 lung cancer cell line, Senexin B significantly slowed tumor growth. In female nude mice with the fat pad injected orthotopically with MDA-MB-468 triple-negative breast cancer (TNBC) cells, 5-day pretreatment with 25 mg/kg daily doses of Senexin B (i.p.) produced strong and sustained inhibition of tumor growth [1].

References:
1.  Cdk8/cdk19 selective inhibitors and their use in anti-metastatic and chemopreventative methods for cancer. Publication number: WO2013116786 A1.
2.  Donald C. Porter, Mengqian Chen, Jiaxin Liang, et al. Abstract PR08: Targeting tumor microenvironment with selective small-molecule inhibitors of CDK8/19.