BS-181 dihydrochloride

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BS-181 dihydrochloride 

BS-181 dihydrochloride 是一种有效的,选择性的 CDK7 抑制剂 (IC50=21 nM),与 Seliciclib (HY-30237) 相比。BS-181 dihydrochloride 抑制 CDK2、CDK5 和 CDK9 的 IC50 值分别为 880 nM、3000 nM 和 4200 nM (不能阻断CDK1、4 和 6)。BS-181 dihydrochloride 抑制一组癌细胞生长 (IC50=11.5 μM-37.3 μM),诱导细胞凋亡 (apoptosis)。BS-181 dihydrochloride 可以用于癌症的相关研究。

BS-181 dihydrochloride

BS-181 dihydrochloride Chemical Structure

CAS No. : 1883548-83-1

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BS-181 dihydrochloride 的其他形式现货产品:

BS-181 BS-181 hydrochloride

生物活性

BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy[1][2].

IC50 & Target[1]

CDK7

21 nM (IC50)

CDK2

880 nM (IC50)

CDK5

3000 nM (IC50)

CDK9

4200 nM (IC50)

体外研究
(In Vitro)

BS-181 dihydrochloride (0-40 μM; 72 hours) inhibits cancer cells growth, it is against Breast cancer cell lines growth with IC50 values ranging from 15.1 μM to 20 μM, it is against Colorectal cancer cell lines growth with IC50 values ranging from 11.5 μM to15.3 μM and is against lung, osteosarcoma, prostate and liver cancer cell lines with IC50 values ranging from 11.5 μM to 37.3 μM, respectively[1].
BS-181 dihydrochloride (0-50 μM; 4 hours) shows inhibition of phosphorylation of the RNA polymerase II C-terminal domain (CTD) at serine 5 (P-Ser5). It down-regulates CDK4 and cyclin D1 expression while does not effect other CDKs and cyclins[1].
BS-181 dihydrochloride (0-50 μM; 24 hours) shows an increase in cells in G1, accompanied by a reduction in cell numbers in S and G2/M at low concentrations. At higher concentrations, however, cells accumulates in the sub-G1, indicative of apoptosis[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Breast cancer cell line: MCF-7, MDA-MB-231, T47D, ZR-75-1, etc
Colorectal cancer cell line: COLO-205, HCT-116, HCT-116 (p53-/-)
Lung cancer cell line: A549, NCI-460
Osteosarcoma cancer cell line: U2OS, SaOS2
Prostate cancer cell line: PC3, LNCaP
Concentration: 0-40 μM
Incubation Time: 72 hours
Result: Had anti-proliferative activities against a panel of cell lines, including breast, lung, prostate and colorectal cancer.

Western Blot Analysis[1]

Cell Line: Breast cancer cell line: MCF-7 cells
Concentration: 0 μM; 25 μM; 50 μM
Incubation Time: 4 hours
Result: Inhibited phosphorylation of CDK7 substrates.

Apoptosis Analysis[1]

Cell Line: Breast cancer cell line: MCF-7 cells
Concentration: 0 μM; 25 μM; 50 μM
Incubation Time: 24 hours
Result: Led cells to G1 arrest and apoptosis.

体内研究
(In Vivo)

BS-181 dihydrochloride (intraperitoneal injection; 10 mg/kg, 20 mg/kg; single dose) is well tolerated in mice without apparent weight altering[1].
BS-181 dihydrochloride (intraperitoneal injection; 5 mg/kg or 10 mg/kg twice daily; total daily doses of 10 mg/kg or 20 mg/kg; 14 days) inhibitstumor growth in a dose-dependent manner. Tumor growth exhibits 25% and 50% reduction compared with the control group, for 10 mg/kg/day and 20 mg/kg/day, respectively[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 7-week old female nu/nu-BALB/c athymic nude mice with MCF-7 cells[1]
Dosage: 5 mg/kg or 10 mg/kg; 10 mg/kg or 20 mg/kg
Administration: Intraperitoneal injection; twice daily or once total daily; 14 days
Result: Inhibited tumor growth significantly.

分子量

453.45

Formula

C22H34Cl2N6

CAS 号

1883548-83-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Ali S et al. The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. Cancer Res. 2009 Aug 1;69(15):6208-15.

    [2]. Wang BY, et al. Selective CDK7 inhibition with BS-181 suppresses cell proliferation and induces cell cycle arrest and apoptosis in gastric cancer. Drug Des Devel Ther. 2016 Mar 16;10:1181-9.

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