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BS-181 hydrochloride

Cat. No. M3504
BS-181 hydrochloride Structure
Synonym:

BS-181 HCl

Size Price Availability Quantity
2mg USD 60  USD60 In stock
5mg USD 95  USD95 In stock
10mg USD 135  USD135 In stock
25mg USD 280  USD280 In stock
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Quality Control & Documentation
Biological Activity

BS-181 hydrochloride is a selective cyclin-dependent kinase inhibitor with an IC50 of 21 nM for the inhibition of CDK-activating kinase. Testing of other CDKs as well as another 69 kinases showed that BS-181 hydrochloride only inhibited CDK2 at concentrations lower than 1 μM, with CDK2 being inhibited 35-fold less potently (IC50 880 nM) than CDK7. In MCF-7 cells, BS-181 hydrochloride inhibited the phosphorylation of CDK7 substrates, promoted cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines.

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. 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.

Customer Product Validations & Biological Datas
Source Drug Des Devel Ther (2016). Figure 1. BS-181
Method Cell migration and invasion assay
Cell Lines BGC 823 cells
Concentrations 1, 10, 20 μM
Incubation Time 24 h
Results As expected, BS-181 significantly inhibited cell migration and invasion ability in a dose-dependent manner
Protocol (for reference only)
Cell Experiment
Cell lines MCF-7 cells
Preparation method Exposing MCF-7 cells to BS-181 for 24 hours. For the determination of cell cycle and apoptosis, staining cells with propidium iodide or labeled with Annexin V-FITC, then acquiring labeled cells within 1 hour, by using the RXP cytomics software on a Beckman Coulter Elite ESP, and using Flow Jo v7.2.5 to analyze the data . For the assessment of CDKs, lysing and analyzing cells by western blotting.
Concentrations Dissolved in DMSO, final concentration ~50 μM
Incubation time 24 hours
Animal Experiment
Animal models MCF-7 cells are established in female nu/nu-BALB/c athymic nude mice
Formulation Prepared in the vehicle of 10% DMSO / 50 mM HCl / 5% Tween 20 / 85% saline.
Dosages 10 or 20 mg/kg
Administration Twice daily by i.p. injection
Chemical Information
Molecular Weight 416.99
Formula C22H32N6.HCl
CAS Number 1397219-81-6
Solubility (25°C) Water 85 mg/mL
DMSO 45 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

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  Catalog
Abmole Inhibitor Catalog




Keywords: BS-181 hydrochloride, BS-181 HCl supplier, CDK, inhibitors, activators


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