生物活性 | Voruciclib hydrochloride is an orally active and selectiveCDKinhibitor withKivalues of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocksCDK9, the transcriptional regulator ofMCL-1. Voruciclib hydrochloride represses expression ofMCL-1in multiple models of diffuse large B-cell lymphoma (DLBCL)[1]. |
IC50& Target[1] | CDK9/CycT1 1.68 nM (Ki) | CDK9/cyc T2 0.626 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) |
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体外研究 (In Vitro) | Voruciclib hydrochloride (0.5-5 μM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes[1]. Kivalues 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].
Western Blot Analysis[1] Cell Line: | U2932, RIVA, OCI-LY10 cells (ABC subtype), NU-DHL-1, SU-DHL-4, SU-DHL-6 cells (GCB subtype) | Concentration: | 0.5 μM, 1 μM, 2 μM, 3 μM, 4 μM, 5 μM | Incubation Time: | 6 hours | Result: | Showed targeted downregulation of MCL-1 in both ABC and GCB subtypes. |
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体内研究 (In Vivo) | Combination of Voruciclib hydrochloride (200 mpk; Oral gavage) and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) leads to enhance tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), and NU-DHL-1 models (five days per week for 3 weeks) of DLBCL[1].
Animal Model: | ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice[1] | Dosage: | 200 mpk | 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) | Result: | Enhanced tumor growth inhibition in U2932, RIVA, SU-DHL-4 and NU-DHL-1 models except in OCI-LY10 model. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : ≥ 250 mg/mL(493.78 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 1.9751 mL | 9.8756 mL | 19.7511 mL | 5 mM | 0.3950 mL | 1.9751 mL | 3.9502 mL | 10 mM | 0.1975 mL | 0.9876 mL | 1.9751 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.11 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.11 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.11 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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