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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3034210-97-1
- 分子式: C30H26N6O3
- 分子量:518.57
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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] |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 3034210-97-1
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分子量 518.57
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CDK7-IN-20 関連分類
HY-151878 関連分類
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