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BS-181 hydrochloride

Cat. No. M3504
BS-181 hydrochloride Structure
Size Price Availability Quantity
5mg USD 100 In stock
10mg USD 180 In stock
50mg USD 550 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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, and showed antitumor effects in vivo.

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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 416.99
Formula C22H32N6.HCl
CAS Number 1397219-81-6
Purity >98%
Solubility DMSO 80 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BS-181 hydrochloride supplier, CDK, inhibitors

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