1. Cell Cycle/DNA Damage
  2. CDK
  3. BS-181 hydrochloride

BS-181 hydrochloride 

Cat. No.: HY-13266A
Handling Instructions

BS-181 hydrochloride 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 hydrochloride Chemical Structure

BS-181 hydrochloride Chemical Structure

CAS No. : 1397219-81-6

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Top Publications Citing Use of Products

    BS-181 hydrochloride purchased from MCE. Usage Cited in: Theranostics. 2017 Apr 20;7(7):1914-1927.

    Effect of TPL on the levels of pAR S515 and related proteins in PCa cells. LNCaP and C4-2/AR-V7 cells are pretreated with TPL or BS-181 for 1 h, and then incubated with R1881 for 4 h.
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    Description

    BS-181 hydrochloride 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[1]

    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)

    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].

    Molecular Weight

    416.99

    Formula

    C₂₂H₃₃ClN₆

    CAS No.

    1397219-81-6

    SMILES

    CC(C1=C(N=C(C=C2NCC3=CC=CC=C3)NCCCCCCN)N2N=C1)C.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    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]

    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 ×width2)/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
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    Keywords:

    BS-181BS181BS 181CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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