1. Cell Cycle/DNA Damage
    Apoptosis
  2. CDK
    Apoptosis
  3. CDKI-73

CDKI-73 

Cat. No.: HY-12445 Purity: 99.58%
Handling Instructions

CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).

For research use only. We do not sell to patients.

CDKI-73 Chemical Structure

CDKI-73 Chemical Structure

CAS No. : 1421693-22-2

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 462 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE CDKI-73

    CDKI-73 purchased from MCE. Usage Cited in: Am J Cancer Res. 2020 Apr 1;10(4):1140-1155. 

    The expression of BRCA1, p-CDK9, CDK9, Bcl-2 proteins, γ-H2AX, cleaved PARP, and cleaved caspase-3 in HO8910 cells treated with CDKI-73.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM). IC50 value: 4 nM/80 nM(Ki/LD50) [1] Target: CDK9 inhibitor in vitro: CDKI-73 was cytotoxic to all of the CLL samples tested (n = 38) with a mean LD50 value of 0.08μM ± 0.10 μM following exposure to drug for 48h. In contrast, normal B-lymphocytes (n = 10) and CD34+ normal bone marrow cells (n = 5) were significantly less susceptible to the cytotoxic effects of CDKI-73. Treatment of CLL cells with 0.1 μM CDKI-73 for 4h inhibited the phosphorylation of cdk9 and ser2 of RNA polymerase II. CDKI-73 induces a rapid loss of MCL1 protein and this is mediated by significant inhibition at the level of gene transcription. However, this inhibition is not restricted to MCL1 as similar reductions in XIAP and CCND2 were also observed following exposure to CDKI-73 for 4h [1]. CDKI-73 rapidly inhibited cellular CDK9 kinase activity and down-regulated the RNAPII phosphorylation. CDK9 shRNA was also found to down-regulate the Mnk1 expression. Both CDKI-73 and CDK9 shRNA decreased anti-apoptotic proteins Mcl-1 and Bcl-2 and induced apoptosis [2]. in vivo: CDKI-73 exhibited a favorable pharmacokinetic profile with oral bioavailability of F = 56% following a single intravenous bolus dose at 2 mg/kg and an oral dose at 10 mg/kg in mice [1].

    IC50 & Target[1]

    CDK2

    3.27 nM (IC50)

    CDK9

    5.78 nM (IC50)

    CDK1

    8.17 nM (IC50)

    CDK4

    8.18 nM (IC50)

    CDK6

    37.68 nM (IC50)

    CDK7

    134.26 nM (IC50)

    Molecular Weight

    394.45

    Formula

    C₁₅H₁₅FN₆O₂S₂

    CAS No.

    1421693-22-2

    SMILES

    CNC1=NC(C)=C(C2=C(F)C=NC(NC3=CC(S(=O)(N)=O)=CC=C3)=N2)S1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 52 mg/mL (131.83 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5352 mL 12.6759 mL 25.3518 mL
    5 mM 0.5070 mL 2.5352 mL 5.0704 mL
    10 mM 0.2535 mL 1.2676 mL 2.5352 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.67 mg/mL (6.77 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.58%

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    Keywords:

    CDKI-73CDKI73CDKI 73CDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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    Product name:
    CDKI-73
    Cat. No.:
    HY-12445
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