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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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

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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CDKI-73
Cat. No.:
HY-12445
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