WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H407248
CAS#: 1449228-40-3
Description: Senexin B is a potent and selective CDK8/19 inhibitor. Senexin B inhibits CDK8/19 in low nanomolar range in vitro and in vivo as an ATP pocket binder, with very high target selectivity as indicated by kinome profiling. It is highly water-soluble, bioavailable, and produces no limiting toxicity upon prolonged administration in mice, at doses that yield plasma concentrations exceeding cellular IC50 by 2-3 orders of magnitude. CDK8/19 inhibition produces chemopotentiating, chemopreventive and anti-metastatic effects in different types of cancer, inhibiting tumor progression by acting both at the tumor cells (the “seed”) and the tumor microenvironment (the “soil”) of cancers.
Hodoodo Cat#: H407248
Name: Senexin B
CAS#: 1449228-40-3
Chemical Formula: C27H26N6O
Exact Mass: 450.22
Molecular Weight: 450.550
Elemental Analysis: C, 71.98; H, 5.82; N, 18.65; O, 3.55
Synonym: Senexin B
IUPAC/Chemical Name: 4-((2-(6-(4-methylpiperazine-1-carbonyl)naphthalen-2-yl)ethyl)amino)quinazoline-6-carbonitrile
InChi Key: VNADJTWHOAMTLY-UHFFFAOYSA-N
InChi Code: InChI=1S/C27H26N6O/c1-32-10-12-33(13-11-32)27(34)23-6-5-21-14-19(2-4-22(21)16-23)8-9-29-26-24-15-20(17-28)3-7-25(24)30-18-31-26/h2-7,14-16,18H,8-13H2,1H3,(H,29,30,31)
SMILES Code: O=C(C1=CC2=CC=C(CCNC3=C4C(C=CC(C#N)=C4)=NC=N3)C=C2C=C1)N5CCN(C)CC5
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Abstract PR08: Targeting tumor microenvironment with selective small-molecule inhibitors of CDK8/19. Donald C. Porter1, Mengqian Chen2, Jiaxin Liang2, Vimala Kaza1, Alexander Chumanevich1, Serena Altilia1, Elena Farmaki3, Marj Pena2, Gary P. Schools2, Ioulia Chatzistamou3, Lawrence T. Friedhoff1, Mark P. Wentland4, Eugenia V. Broude2, Hippokratis Kiaris3, and Igor B. Roninson2. Abstracts: AACR Special Conference on Cellular Heterogeneity in the Tumor Microenvironment; February 26 — March 1, 2014; San Diego, CA
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The following data is based on the product molecular weight 450.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1. Roninson, I.B., Porter, D.C., and Wentland, M.P. Cdk8-cdk19 selective inhibitors and their use in anti-metastatic and chemopreventative methods for cancer. (2016).
2. McDermott, M.S., Chumanevich, A.A., Lim, C.-U., et al. Inhibition of CDK8 mediator kinase suppresses estrogen dependent transcription and the growth of estrogen receptor positive breast cancer. Oncotarget 8(8), 12558-12575 (2017).
3. Amirhosseini, M., Bernhardsson, M., Lång, P., et al. Cyclin-dependent kinase 8/19 inhibition suppresses osteoclastogenesis by downregulating RANK and promotes osteoblast mineralization and cancellous bone healing. J. Cell. Physiol. 234(9), 16503-16516 (2019).