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.
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- CAS No.: 3034210-97-1
- 화학식: C30H26N6O3
- 분자량:518.57
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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) |
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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 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.
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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분자량 518.57
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK7-IN-20 Related Classifications
HY-151878 Related Classifications
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