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

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

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

KB-0742 Chemical Structure

KB-0742 Chemical Structure

CAS No. : 2416873-83-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of KB-0742:

KB-0742 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE KB-0742

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

  • Purity & Documentation

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Description

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

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

KB-0742 Related Antibodies

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].

MedChemExpress (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

287.40

Formula

C16H25N5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N[C@@H]1C[C@@H](NC2=CC(C(CC)CC)=NC3=CC=NN23)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 175 mg/mL (608.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4795 mL 17.3974 mL 34.7947 mL
5 mM 0.6959 mL 3.4795 mL 6.9589 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.38%

SDS (251 KB)

COA (252 KB) HNMR (249 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4795 mL 17.3974 mL 34.7947 mL 86.9868 mL
5 mM 0.6959 mL 3.4795 mL 6.9589 mL 17.3974 mL
10 mM 0.3479 mL 1.7397 mL 3.4795 mL 8.6987 mL
15 mM 0.2320 mL 1.1598 mL 2.3196 mL 5.7991 mL
20 mM 0.1740 mL 0.8699 mL 1.7397 mL 4.3493 mL
25 mM 0.1392 mL 0.6959 mL 1.3918 mL 3.4795 mL
30 mM 0.1160 mL 0.5799 mL 1.1598 mL 2.8996 mL
40 mM 0.0870 mL 0.4349 mL 0.8699 mL 2.1747 mL
50 mM 0.0696 mL 0.3479 mL 0.6959 mL 1.7397 mL
60 mM 0.0580 mL 0.2900 mL 0.5799 mL 1.4498 mL
80 mM 0.0435 mL 0.2175 mL 0.4349 mL 1.0873 mL
100 mM 0.0348 mL 0.1740 mL 0.3479 mL 0.8699 mL
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KB-0742 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KB-07422416873-83-9KB0742KB 0742CDKCyclin dependent kinaseCDK9oralanticancerCRPCSer2Ser7Ser5antiproliferativeInhibitorinhibitorinhibit

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