Voruciclib
Based on 1 Customer Validation
Voruciclib is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
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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。
- 純度: 99.76%
- CAS 番号: 1000023-04-0
- 分子式: C22H19ClF3NO5
- 分子量:469.84
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
生物活性
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CDK9/cyc T2 0.626 nM (Ki) |
CDK9/CycT1 1.68 nM (Ki) |
CDK6/cycD1 2.92 nM (Ki) |
CDK4/Cyc D1 3.96 nM (Ki) |
CDK1/cycB 5.4 nM (Ki) |
CDK1/cyc A 9.1 nM (Ki) |
Voruciclib (0.5-5 μM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes[1].
Ki values for each target such as CDK9/cyc T2, CDK9/cyc T1, CDK6/cyc D1, CDK4/cyc D1, CDK1/cyc B, and CDK1/cyc A for Voruciclib hydrochloride are 0.626 nM, 1.68 nM, 2.92 nM, 3.96 nM, 5.4 nM, 9.1 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U2932, RIVA, OCI-LY10 cells (ABC subtype), NU-DHL-1, SU-DHL-4, SU-DHL-6 cells (GCB subtype)
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Concentration:0.5 µM, 1 µM, 2 µM, 3 µM, 4 µM, 5 µM
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Incubation Time:6 hours
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Result:Showed targeted downregulation of MCL-1 in both ABC and GCB subtypes.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice
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Dosage:200 mpk
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Administration:Oral gavage; U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), OCI-LY10 (six days per week for 2 weeks), NU-DHL-1 (five days per week for 3 weeks)
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Result:Enhanced tumor growth inhibition in U2932, RIVA, SU-DHL-4 and NU-DHL-1 models except in OCI-LY10 model.
化学情報
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CAS 番号 1000023-04-0
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性状 Solid
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分子量 469.84
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分子式 C22H19ClF3NO5
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Color Light yellow to yellow
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SMILES
O=C1C=C(C2=CC=C(C(F)(F)F)C=C2Cl)OC3=C([C@H]4[C@H](CO)N(C)CC4)C(O)=CC(O)=C13
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : 50 mg/mL (106.42 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (393 KB)
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- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1284 mL | 10.6419 mL | 21.2838 mL | 53.2096 mL |
| 5 mM | 0.4257 mL | 2.1284 mL | 4.2568 mL | 10.6419 mL | |
| 10 mM | 0.2128 mL | 1.0642 mL | 2.1284 mL | 5.3210 mL | |
| 15 mM | 0.1419 mL | 0.7095 mL | 1.4189 mL | 3.5473 mL | |
| 20 mM | 0.1064 mL | 0.5321 mL | 1.0642 mL | 2.6605 mL | |
| 25 mM | 0.0851 mL | 0.4257 mL | 0.8514 mL | 2.1284 mL | |
| 30 mM | 0.0709 mL | 0.3547 mL | 0.7095 mL | 1.7737 mL | |
| 40 mM | 0.0532 mL | 0.2660 mL | 0.5321 mL | 1.3302 mL | |
| 50 mM | 0.0426 mL | 0.2128 mL | 0.4257 mL | 1.0642 mL | |
| 60 mM | 0.0355 mL | 0.1774 mL | 0.3547 mL | 0.8868 mL | |
| 80 mM | 0.0266 mL | 0.1330 mL | 0.2660 mL | 0.6651 mL | |
| 100 mM | 0.0213 mL | 0.1064 mL | 0.2128 mL | 0.5321 mL |