KB-0742 dihydrochloride
Based on 3 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.77%
- No. CAS: 2416874-75-2
- Fòrmula: C16H27Cl2N5
- Peso molecular:360.33
-
Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
HY-112088
AZD4573CDK9 Inhibitor -
HY-50767
PalbociclibCDK4/6 Inhibitor -
HY-10492
DinaciclibCDK2/5/9 Inhibitor -
HY-103712A
Samuraciclib hydrochlorideCDK7 Inhibitor -
HY-10005
FlavopiridolCDK Inhibitor -
HY-A0065
Palbociclib isethionateCDK4/6 Inhibitor -
HY-80013
THZ1CDK7 Inhibitor -
HY-160701
CirtociclibCDK2 Inhibitor -
HY-10583
Y-27632 dihydrochlorideROCK Inhibitor -
HY-15889
AMG 925FLT3/CDK4 Inhibitor -
HY-130250
SR-4835CDK12/13 Inhibitor -
HY-10580
GSK 3 Inhibitor IXATP-Competitive Inhibitor
Publications Citing Use of MedChemExpress (MCE) KB-0742 dihydrochloride
More
Actividad biológica
Descripciòn
|
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 D 3130 nM (IC50) |
CDK6/cyclinD1 3950 nM (IC50) |
CDK8/cyclin C >10000 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. Further protocols information, click here.
-
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
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).
Chemical Information
-
No. CAS 2416874-75-2
-
Appearance Solid
-
Peso molecular 360.33
-
Fòrmula C16H27Cl2N5
-
Color Light yellow to yellow
-
SMILES
N[C@@H]1C[C@@H](NC2=CC(C(CC)CC)=NC3=CC=NN23)CC1.[H]Cl.[H]Cl
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (3)
-
Journal Impact Factor
-
Most Recent
Solvente y solubilidad
In Vitro:
H2O : 100 mg/mL (277.52 mM; Need ultrasonic)
DMSO : 62.5 mg/mL (173.45 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (277.52 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocolo
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureza y Documentación
-
Ficha de datos (283 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.7752 mL | 13.8762 mL | 27.7523 mL | 69.3808 mL |
| 5 mM | 0.5550 mL | 2.7752 mL | 5.5505 mL | 13.8762 mL | |
| 10 mM | 0.2775 mL | 1.3876 mL | 2.7752 mL | 6.9381 mL | |
| 15 mM | 0.1850 mL | 0.9251 mL | 1.8502 mL | 4.6254 mL | |
| 20 mM | 0.1388 mL | 0.6938 mL | 1.3876 mL | 3.4690 mL | |
| 25 mM | 0.1110 mL | 0.5550 mL | 1.1101 mL | 2.7752 mL | |
| 30 mM | 0.0925 mL | 0.4625 mL | 0.9251 mL | 2.3127 mL | |
| 40 mM | 0.0694 mL | 0.3469 mL | 0.6938 mL | 1.7345 mL | |
| 50 mM | 0.0555 mL | 0.2775 mL | 0.5550 mL | 1.3876 mL | |
| 60 mM | 0.0463 mL | 0.2313 mL | 0.4625 mL | 1.1563 mL | |
| 80 mM | 0.0347 mL | 0.1735 mL | 0.3469 mL | 0.8673 mL | |
| 100 mM | 0.0278 mL | 0.1388 mL | 0.2775 mL | 0.6938 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
KB-0742 dihydrochloride Related Classifications
HY-137478A Related Classifications
Powered by Bioz