1. Cell Cycle/DNA Damage
  2. CDK
  3. KB-0742 dihydrochloride

KB-0742 dihydrochloride 

Cat. No.: HY-137478A Purity: 99.63%
Handling Instructions

KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.

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

KB-0742 dihydrochloride Chemical Structure

KB-0742 dihydrochloride Chemical Structure

CAS No. : 2416874-75-2

Size Price Stock Quantity
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity[1].

IC50 & Target[1]

CDK9/cyclinT1

6 nM (IC50)

In Vitro

KB-0742 (6 hours; 0.1-10 μM; 22Rv1 cells) treatment significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5. Global androgen receptor (AR)-FL and AR-V protein levels are significantly reduced starting at 6 h treatment time, which is accompanied by the reduction of phospho-AR levels (Ser81)[1].
KB-0742 (48-72 hours) treatment shows cytostatic effects in prostate cancer and leukemia cell lines. KB-0742 shows antiproliferative activity with GR50s of 0.183 μM and 0.288 μM for 22Rv1 cells and MV-4-11 AML cells, respectively[1].
In 22Rv1 cells, KB-0742 rapidly downregulates nascent transcription, preferentially depleting short half-life transcripts and AR-driven oncogenic programs[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 10 μM
Incubation Time: 6 hours
Result: Significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5.
In Vivo

KB-0742 (3-30 mg/kg; p.o.; daily; over 21 days) is well tolerated even at high dose, while significantly reducing tumor burden in 22Rv1 human prostate cancer cell line-derived xenograft (CDX) models[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CB17-SCID mice injected with 22Rv1 human prostate cancer cells[1]
Dosage: 3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration: p.o.; daily; over 21 days
Result: Significantly reduced tumor growth in castration-resistant prostate cancer (CRPC).
Molecular Weight

360.33

Formula

C₁₆H₂₇Cl₂N₅

CAS No.

2416874-75-2

SMILES

N[[email protected]@H]1C[[email protected]@H](NC2=CC(C(CC)CC)=NC3=CC=NN23)CC1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (173.45 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7752 mL 13.8762 mL 27.7523 mL
5 mM 0.5550 mL 2.7752 mL 5.5505 mL
10 mM 0.2775 mL 1.3876 mL 2.7752 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: ≥ 2.08 mg/mL (5.77 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.77 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.77 mM); Clear solution

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

KB-0742KB0742KB 0742CDKCyclin dependent kinaseCDK9oralanticancerCRPCSer2Ser7Ser5antiproliferativeInhibitorinhibitorinhibit

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KB-0742 dihydrochloride
Cat. No.:
HY-137478A
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