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BS-181 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BS-181 dihydrochloride图片
CAS NO:1883548-83-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

BS-181 dihydrochloride is a potent and selectiveCDK7inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also againstCDK2,CDK5andCDK9withIC50values of 880 nM, 3000 nM and 4200 nM, respectively (fails to blockCDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel ofcancercells growth (IC50=11.5 μM-37.3 μM) and induces cellapoptosis. BS-181 dihydrochloride has the potential for the research ofcancertherapy[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 IC50values ranging from 15.1 μM to 20 μM, it is against Colorectal cancer cell lines growth with IC50values ranging from 11.5 μM to15.3 μM and is against lung, osteosarcoma, prostate and liver cancer cell lines with IC50values 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].

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].

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.