Senexin B
- CAS No.
- 1449228-40-3
- Chemical Name:
- Senexin B
- Synonyms
- Senexin B;SNX2-1-165;Senexin B (SNX2-1-165);Senexin B, 10 mM in DMSO;4-(2-(6-(4-methylpiperazine-1-carbonyl)naphthalen-2-yl)ethylamino)quinazoline-6-carbonitrile;6-Quinazolinecarbonitrile, 4-[[2-[6-[(4-methyl-1-piperazinyl)carbonyl]-2-naphthalenyl]ethyl]amino]-
- CBNumber:
- CB13355337
- Molecular Formula:
- C27H26N6O
- Molecular Weight:
- 450.53
- MDL Number:
- MFCD31544331
- MOL File:
- 1449228-40-3.mol
| Boiling point | 724.8±60.0 °C(Predicted) |
|---|---|
| Density | 1.32±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | >22.6mg/mL in DMSO |
| form | Powder |
| pka | 6.74±0.10(Predicted) |
| color | White to off-white |
| FDA UNII | E2X758P2BZ |
Senexin B price More Price(11)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 28459 | Senexin B | 1449228-40-3 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 28459 | Senexin B | 1449228-40-3 | 25mg | $533 | 2024-03-01 | Buy |
| Cayman Chemical | 28459 | Senexin B | 1449228-40-3 | 5mg | $139 | 2024-03-01 | Buy |
| Cayman Chemical | 28459 | Senexin B | 1449228-40-3 | 10mg | $243 | 2024-03-01 | Buy |
| AK Scientific | 0870DV | SenexinB | 1449228-40-3 | 5mg | $252 | 2021-12-16 | Buy |
Senexin B Chemical Properties,Uses,Production
Uses
Senexin B (SNX2-1-165; BCD-115) is a potent, highly water-soluble and bioavailable CDK8/19 inhibitor, with Kds of 140 nM for CDK8 and 80 nM for CDK19.
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[1]. Senexin B suppresses tumor growth and augmentes the effects of fulvestrant in ER-positive breast cancer xenografts[2].
IC 50
CDK19: 80 nM (Kd); CDK8: 140 nM (Kd)
References
[1] Porter D, et al. Abstract PR08: Targeting tumor microenvironment with selective small-molecule inhibitors of CDK8/19. Abstracts: AACR Special Conference on Cellular Heterogeneity in the Tumor Microenvironment; 2014 Feb 26-Mar 1; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2015;75(1 Suppl):Abstract nr PR08. doi:10.1158/1538-7445.CHTME14-PR08
[2] McDermott MS, et al. Inhibition of CDK8 mediator kinase suppresses estrogen dependent transcription and the growth of estrogen receptor positive breast cancer. Oncotarget. 2017 Feb 21;8(8):12558-12575. DOI:10.18632/oncotarget.14894
[3] CDK8-CDK19 selective inhibitors and their use in anti-metastatic and chemopreventative methods for cancer. US 9321737 B2
Senexin B Preparation Products And Raw materials
Raw materials
Preparation Products
Senexin B Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30230 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24727 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38630 | 58 | |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Shaanxi Cuikang Pharmaceutical Technology Co., Ltd | +8618791163155 | 18791163155@163.com | China | 3558 | 58 |
| Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 5221 | 58 |
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2922 | 55 |
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