BS-181 hydrochloride
- Product Name
- BS-181 hydrochloride
- CAS No.
- 1092443-52-1
- Chemical Name
- BS-181 hydrochloride
- Synonyms
- BS 181;CS-507;CS-2137;BS-181 HCl;BS-181 free base;BS-181 hydrochloride;N5-(6-Aminohexyl)-3-isopropyl-N7-benzylpyrazolo[1,5-a]pyrimidine-5,7-diamine;Pyrazolo[1,5-a]pyrimidine-5,7-diamine, N5-(6-aminohexyl)-3-(1-methylethyl)-N7-(phenylmethyl)-;5-N-(6-aminohexyl)-7-N-benzyl-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine,hydrochloride
- CBNumber
- CB42561462
- Molecular Formula
- C22H32N6
- Formula Weight
- 380.53
- MOL File
- 1092443-52-1.mol
BS-181 hydrochloride Property
- Density
- 1.16
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Powder
- pka
- 10.62±0.10(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 17996
- Product name
- BS-181
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $35
- Updated
- 2021/12/16
- Product number
- 17996
- Product name
- BS-181
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $158
- Updated
- 2021/12/16
- Product number
- 17996
- Product name
- BS-181
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $280
- Updated
- 2021/12/16
- Product number
- 17996
- Product name
- BS-181
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $963
- Updated
- 2021/12/16
- Product number
- KIN0000936
- Product name
- BS-181 HYDROCHLORIDE
- Purity
- 95.00%
- Packaging
- 10MG
- Price
- $1006.58
- Updated
- 2021/12/16
BS-181 hydrochloride Chemical Properties,Usage,Production
Uses
BS-181 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, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy[1][2].
Definition
ChEBI: N5-(6-aminohexyl)-N7-(phenylmethyl)-3-propan-2-ylpyrazolo[1,5-a]pyrimidine-5,7-diamine is a pyrazolopyrimidine.
in vivo
BS-181 (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. |
IC 50
CDK7/CycH/MAT1: 0.021 μM (IC50); CDK2/Cyc E: 0.88 μM (IC50); CDK5/p35NCK: 3 μM (IC50); CDK9/cycT: 4.2 μM (IC50); CDK1/cycB: 8.1 μM (IC50); CDK4/Cyc D1: 33 μM (IC50); CDK6/cycD1: 47 μM (IC50)
References
[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. DOI:10.1158/0008-5472.CAN-09-0301
[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. DOI:10.2147/DDDT.S86317
BS-181 hydrochloride Preparation Products And Raw materials
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View Lastest Price from BS-181 hydrochloride manufacturers
- Product
- BS-181 hydrochloride 1092443-52-1
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- Min98% HPLC
- Supply Ability
- g/kg/ton
- Release date
- 2019-12-30