KB-0742
Based on 3 publication(s) in Google Scholar
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.
- Purity: 99.63%
- CAS No.: 2416873-83-9
- Formula: C16H25N5
- Molecular Weight:287.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) KB-0742
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Biological Activity
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CDK9/cyclinT1 6 nM (IC50) |
cdk2/cyclin A 397 nM (IC50) |
Cdk5/p25 1820 nM (IC50) |
CDK7/cyclin H 1510 nM (IC50) |
CDK3/Cyclin E 1420 nM (IC50) |
CDK1/cyclin A 2980 nM (IC50) |
Cdk4/cyclin D1 3130 nM (IC50) |
CDK6/cyclinD1 3950 nM (IC50) |
CDK8/cyclin C >10000 () |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-20 | GI50 |
0.6 μM
Compound: 28
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Cytotoxicity against human BT-20 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
Cytotoxicity against human BT-20 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
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[PMID: 37967851] |
| BT-20 | IC50 |
0.97 μM
Compound: 28
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Cytotoxicity against human BT-20 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
Cytotoxicity against human BT-20 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
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[PMID: 37967851] |
| BT-549 | GI50 |
0.8 μM
Compound: 28
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Cytotoxicity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
Cytotoxicity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
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[PMID: 37967851] |
| BT-549 | IC50 |
0.94 μM
Compound: 28
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Cytotoxicity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
Cytotoxicity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
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[PMID: 37967851] |
| Hs-578T | GI50 |
1.06 μM
Compound: 28
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Cytotoxicity against human Hs-578T cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
Cytotoxicity against human Hs-578T cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
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[PMID: 37967851] |
| Hs-578T | IC50 |
1.23 μM
Compound: 28
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Cytotoxicity against human Hs-578T cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
Cytotoxicity against human Hs-578T cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
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[PMID: 37967851] |
| MDA-MB-231 | GI50 |
0.8 μM
Compound: 28
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Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
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[PMID: 37967851] |
| MDA-MB-231 | IC50 |
0.88 μM
Compound: 28
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Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by fluorescence microscopic analysis
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[PMID: 37967851] |
| T-cell | IC50 |
0.006 μM
Compound: 91
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Inhibition of CDK9/Cyclin T (unknown origin)
Inhibition of CDK9/Cyclin T (unknown origin)
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[PMID: 38852339] |
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.
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Cell Line:22Rv1 cells
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Concentration:0.1 μM, 0.5 μM, 1 μM, 10 μM
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Incubation Time:6 hours
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Result:Significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CB17-SCID mice injected with 22Rv1 human prostate cancer cells[1]
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Dosage:3 mg/kg, 10 mg/kg, and 30 mg/kg
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Administration:p.o.; daily; over 21 days
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Result:Significantly reduced tumor growth in castration-resistant prostate cancer (CRPC).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2416873-83-9
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Appearance Solid
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Molecular Weight 287.40
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Formula C16H25N5
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Color White to off-white
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SMILES
N[C@@H]1C[C@@H](NC2=CC(C(CC)CC)=NC3=CC=NN23)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. André Richters, et al. Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors. Cell Chem Biol. 2020 Oct 20;S2451-9456(20)30380-9. [Content Brief]
[2]. Freeman DB, et al. Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers. J Med Chem. 2023 Dec 14;66(23):15629-15647. [Content Brief]
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 |
KB-0742 Related Classifications
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