CDK7-IN-20
CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC50 value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research.
For research use only. We do not sell to patients.
- CAS No.: 3034210-97-1
- Formula: C30H26N6O3
- Molecular Weight:518.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CDK7 4 nM (IC50) |
CDK1 3375 nM (IC50) |
CDK2 823 nM (IC50) |
CDK3 1837 nM (IC50) |
CDK5 >10,000 nM (IC50) |
CDK6 950 nM (IC50) |
CDK9 526 nM (IC50) |
CDK12 >10,000 nM (IC50) |
GSK3β 148 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
13 μM
Compound: B2
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Cytotoxicity against human THP-1 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
Cytotoxicity against human THP-1 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
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[PMID: 36384292] |
In Vitro
In Madin-Darby canine kidney (MDCK) cells, CDK7-IN-20 (Compound B2; 1-3 μM; from day 4 to day 12) shows high potency to inhibit cyst growth and exhibited lower cytotoxicity than THZ1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
ADME Profiles of CDK7-IN-20 (Compound B2)a[1].
| CDK7-IN-20 (Compound B2) | ||
| parameters | i.v. 5 mg/kg | s.c. 5 mg/kg |
| AUClast (h·ng/mL) | 26,937 | 17,280 |
| AUCIFN_obs (h·ng/mL) | 31,698 | 17,411 |
| t1/2 (h) | 17.8 | 3.4 |
| Tmax (h) | 0.5 | |
| Cmax (h) | 3806 | |
| Cl_obs (mL/min/kg) | 2.80 | |
| Vss_obs (mL/kg) | 1275 | |
| MRTIFN_obs (h) | 10.2 | 4.8 |
| F (%) | 64.2 | |
| plasma protein binding (bound%)b | >99 | |
| permeability of Caco-2 A to B Papp (10–6 cm/s)/B to A Papp (10–6 cm/s)/efflux ratioc | <0.133/6.370/>48.0 |
bPlasma from mouse. PPB was tested at 1 and 10 μM substrate concentrations.
bCaco-2 membrane permeability at 10 μM substrate concentrations. The value of 0.133 was determined by quantitative limit (1.0 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Neonatal Pkd1flox/flox:Ksp-Cre mice[1]
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Dosage:5 mg/kg
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Administration:Subcutaneous administration; once daily; for 6 days
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Result:Significantly reduced the kidney size and cyst formation of the ADPKD mice.
Chemical Information
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CAS No. 3034210-97-1
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Molecular Weight 518.57
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Formula C30H26N6O3
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SMILES
C=CC(NC1=CC=C(C=C1)C(NC2=NNC3=C2C=C(C=C3)C4=CC(NC[C@H](C5=CC=CC=C5)O)=CN=C4)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK7-IN-20 Related Classifications
HY-151878 Related Classifications
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