1. Cell Cycle/DNA Damage
  2. CDK

BS-181 

Cat. No.: HY-13266 Purity: 99.72%
Data Sheet SDS Handling Instructions

BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

For research use only. We do not sell to patients.
BS-181 Chemical Structure

BS-181 Chemical Structure

CAS No. : 1092443-52-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $198 In-stock
5 mg $180 In-stock
10 mg $280 In-stock
50 mg $820 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

IC50 & Target

IC50: 21 nM (CDK7)[1]

In Vitro

BS-181 promotes cell cycle arrest and inhibits cancer cell growth, and growth is inhibited for all cell lines tested, with IC50 values ranging from 11.5 to 37 μM. BS-181 inhibits RB phosphorylation at Ser795 and Ser821 with an apparent IC50 of 15 μM, similar to the IC50 obtained for P-Ser2 inhibition. BS-181 treatment of MCF-7 cells leads to G1 arrest at and apoptosis[1]. BS-181 inhibits GC cell and normal gastric epithelial RGM-1 cell line growth with inhibitory concentration (IC50) 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[2].

In Vivo

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[1]. 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[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.6279 mL 13.1396 mL 26.2791 mL
5 mM 0.5256 mL 2.6279 mL 5.2558 mL
10 mM 0.2628 mL 1.3140 mL 2.6279 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

Cell viability is detected using Cell Counting Kit (CCK-8 kit) according to supplier’s introductions. Briefly, BGC823 cells are seeded at 104 cells per well for 48 hours with or without BS-181. Then, the absorbance is detected at 450 nm (reference at 650 nm) in each well. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

BS-181 is prepared in 10% dimethyl sulfoxide/50 mM HCl/5% Tween 20/85% saline.

In total, 5×106 BGC823 cells (0.1 mL) are injected subcutaneously into the flank of the mice. Tumor measurements are performed two times per week, and volumes are calculated using the formula: tumor size=(length [mm] × width2 [mm])/2. Finally, 30 mice (tumor volume 100-200 mm3) are selected and randomLy assigned into three groups. As previously described, BS-181 is prepared in 10% dimethyl sulfoxide/50 mM HCl/5% Tween 20/85% saline. Micereceive BS-181 injection (ip) twice daily at indicated doses (BS-181 [10 mg/kg/d or 20 mg/kg/d] or roscovitine [20 mg/kg/d]) for a total of 14 days. Control mice are injected with vehicles. Animal weights and tumor volume are measured each day throughout the 14-day treatment. In addition, all rats are kept for another 30 days for survival observation. Mice are injected intraperitoneally twice daily with BS-181 at 5 mg/kg or 10 mg/kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

380.53

Formula

C₂₂H₃₂N₆

CAS No.

1092443-52-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
BS-181
Cat. No.:
HY-13266
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