CDK/HDAC-IN-3
Based on 1 Customer Validation
CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.60%
- CAS. Nr.: 2944087-54-9
- Formel: C24H18Cl2N6O3
- Molecular Weight:509.34
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Speicherung:Powder -20°C, 3 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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 98.32 nM (CDK9), 98.85 nM (CDK12), 100 nM (CDK13), 62.12 nM (HDAC1), 93.28nM (HDAC2) and 82.87 nM (HDAC3), 0.72 μM (U937 cell), 1.43μM (HL-60 cell), 1.63μM (SKNO-1 cell) and 0.89 μM (Kaumi-1 cell)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | IC50 |
>20 μM
Compound: 33a
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Antiproliferative activity against HEK293T cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against HEK293T cells incubated for 72 hrs by CCK8 assay
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[PMID: 36736154] |
| HL-60 | IC50 |
1.43 μM
Compound: 33a
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Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CCK8 assay
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[PMID: 36736154] |
| Kasumi 1 | IC50 |
0.89 μM
Compound: 33a
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Antiproliferative activity against human Kasumi 1 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human Kasumi 1 cells incubated for 72 hrs by CCK8 assay
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[PMID: 36736154] |
| U-937 | IC50 |
0.72 μM
Compound: 33a
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Antiproliferative activity against human U-937 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human U-937 cells incubated for 72 hrs by CCK8 assay
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[PMID: 36736154] |
In Vitro
CDK/HDAC-IN-3 (compound 33a) (1μM) has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM, respectively[1].
CDK/HDAC-IN-3 (0.5 μM, 1.0 μM) significantly induces differentiation of leukemic stem-like cells and inhibits AML proliferation[1].
CDK/HDAC-IN-3 (0.5 μM, 1.0 μM, 2.0 μM) significantly induced differentiation of LSCs[1].
CDK/HDAC-IN-3 has inhibitory effect for U937, HL-60, SKNO-1 and Kaumi-1 cell with IC50 values of 0.72 μM, 1.43μM, 1.63μM and 0.89 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Human leukemia cell lines Kaumi-1, Skno-1, HL-60 and U937
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Concentration:At different concentrations
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Incubation Time:72 h
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Result:Showed strong growth inhibitory potency against AML cells.
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Cell Line:HL-60 cell
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Concentration:0, 30, 100, 300, 1000 nM
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Incubation Time:6 h
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Result:Inhibited the downstream signaling of HDAC and CDK9 in a dose-dependent manner.
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Cell Line:HL-60 and U937 cell
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Concentration:0.2, 0.5, 1.0, 2.0 μM
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Incubation Time:48 h
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Result:Induced apoptosis of AML cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley male rats (220-350 g)[1]
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Dosage:5 mg/kg and 25 mg/kg
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Administration:IV and PO
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Result:
PK parameters i.v (5 mg/Kg) p.o (25 mg/Kg) Cmax(ng/L) 3644.00 1426.00 T1/2(h) 0.11 1.37 TMax(h) NA 0.75 Clearance (mL/h/kg) 5307.00 1726.00 MRT (h) 0.39 1.27 AUC (ng.h/mL) 836.00 2368.00 F% NA 56.70%
Chemical Information
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CAS. Nr. 2944087-54-9
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Appearance Solid
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Molecular Weight 509.34
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Formel C24H18Cl2N6O3
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Color White to yellow
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SMILES
NC1=C(C=CC=C1)NC(C2=CC=C(C=C2)NC(C3=NNC=C3NC(C4=C(C=CC=C4Cl)Cl)=O)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 125 mg/mL (245.42 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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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.
Reinheit & Dokumentation
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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)
Verweise
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 | 1.9633 mL | 9.8166 mL | 19.6333 mL | 49.0831 mL |
| 5 mM | 0.3927 mL | 1.9633 mL | 3.9267 mL | 9.8166 mL | |
| 10 mM | 0.1963 mL | 0.9817 mL | 1.9633 mL | 4.9083 mL | |
| 15 mM | 0.1309 mL | 0.6544 mL | 1.3089 mL | 3.2722 mL | |
| 20 mM | 0.0982 mL | 0.4908 mL | 0.9817 mL | 2.4542 mL | |
| 25 mM | 0.0785 mL | 0.3927 mL | 0.7853 mL | 1.9633 mL | |
| 30 mM | 0.0654 mL | 0.3272 mL | 0.6544 mL | 1.6361 mL | |
| 40 mM | 0.0491 mL | 0.2454 mL | 0.4908 mL | 1.2271 mL | |
| 50 mM | 0.0393 mL | 0.1963 mL | 0.3927 mL | 0.9817 mL | |
| 60 mM | 0.0327 mL | 0.1636 mL | 0.3272 mL | 0.8181 mL | |
| 80 mM | 0.0245 mL | 0.1227 mL | 0.2454 mL | 0.6135 mL | |
| 100 mM | 0.0196 mL | 0.0982 mL | 0.1963 mL | 0.4908 mL |
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