1397219-81-6
BS-181 (hydrochloride)
CAS: 1397219-81-6
Molecular Formula: C22H33ClN6
1397219-81-6 - Names and Identifiers
| Name | BS-181 (hydrochloride) |
| Synonyms | BS181 CS-979 BS 181 BS-181 HCl BS-181 (hydrochloride) N5-(6-aminohexyl)-N7-benzyl-3-isopropylpyrazolo[1,5-a]pyrimidine-5,7-diamine hydrochloride |
| CAS | 1397219-81-6 |
1397219-81-6 - Physico-chemical Properties
| Molecular Formula | C22H33ClN6 |
| Molar Mass | 416.99062 |
| Solubility | 10 mM in DMSO |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| In vitro study | BS-181 promotes cell cycle arrest and inhibits cancer cell growth, and growth is inhibited for all cell lines tested, with IC 50 values ranging from 11.5 to 37 μM. BS-181 inhibits RB phosphorylation at Ser 795 and Ser 821 with an apparent IC 50 of 15 μM, similar to the IC 50 obtained for P-Ser2 inhibition. BS-181 treatment of MCF-7 cells leads to G1 arrest at and apoptosis. BS-181 inhibits GC cell and normal gastric epithelial RGM-1 cell line growth with inhibitory concentration (IC 50 ) ranging from 17 to 22 μM and 6.5 μM, respectively. BS-181 significantly inhibits cell migration and invasion ability in a dose-dependent manner. |
| In vivo study | BS-181 (5 mg/kg, 10 mg/kg, i.p.) inhibits the growth of MCF-7 tumors in nude mice. Intravenous (i.v) and i.p administration of 10 mg/kg BS-181 shows rapid clearance. BS-181 (10 mg/kg/d or 20 mg/kg/d, i.p.) significantly inhibits the growth of tumor in a dose-dependent manner compared to the control group. |
1397219-81-6 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.398 ml | 11.991 ml | 23.981 ml |
| 5 mM | 0.48 ml | 2.398 ml | 4.796 ml |
| 10 mM | 0.24 ml | 1.199 ml | 2.398 ml |
| 5 mM | 0.048 ml | 0.24 ml | 0.48 ml |
Last Update：2024-01-02 23:10:35
1397219-81-6 - Reference Information
| biological activity | BS-181 hydrochloride is a highly selective CDK7 inhibitor with an IC50 value of 21 nM, and its selectivity to CDK7 is more than 40 times that to CDK1,2,4,5,6 and 9. |
| target | CDK7/CycH/MAT1 0.021 μ m (IC 50 ) CDK2/Cyc E 0.88 μ m (IC 50 ) CDK5/p35NCK 3 μ m (IC 50) CDK9/CYCT 4.2 μ m (IC 50) CDK1/CYCB 8.1 μ m (IC 50) CDK4/CyCD1 33 μ m (IC 50) CDK6/CYCD1 47 μ m (IC 50 ) |
| in vitro study | BS-181 promotes cell cycle arrest and inhibits cell growth, and growth is inhibited for all cell lines examined, with IC 50 values ranging from 11.5 to 37 μ m. BS-181 inhibits RB phosphorylation at Ser 795 and Ser 821 with an apparent IC 50 of 15 μ m, similar to the IC 50 obtained for P-Ser2 inhibition. BS-181 treatment of MCF-7 cells led to G1 arrest at and apoptosis. BS-181 inhibits GC cell and normal gastric epithelial RGM-1 cell line growth with inhibitory concentration (IC 50 ) ranging from 17 to 22 μ m and 6.5 μ m, respectively. BS-181 significantly inhibits cell migration and invasion ability in a pose-dependent manner. |
| in vivo study | BS-181 (5 mg/kg, 10 mg/kg, I. p.) inhibits the growth of MCF-7 tumours in nude mice. Intravenous (I. v) and I. p administration of 10 mg/kg BS-181 shows rapid clearance. BS-181 (10 mg/kg/d or 20 mg/kg/d, I. p.) significantly inhibits the growth of tumor in a dose-dependent banner compared to the control group. |
Last Update：2024-04-09 20:49:11
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