2. Cell Cycle/DNA Damage
  3. CDK
  4. Voruciclib

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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Voruciclib

Voruciclib 構造式

CAS 番号 : 1000023-04-0

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 362 在庫あり
Solution
10 mM * 1 mL in DMSO USD 362 在庫あり
Solid
1 mg $180 在庫あり
5 mg $350 在庫あり
10 mg $550 在庫あり
50 mg $1650 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

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Other Forms of Voruciclib:

Voruciclib 関連抗体

Top Publications Citing Use of Products

CDK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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製品説明

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)[1].

IC50 & Target[1]

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)

体外実験

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.

Voruciclib 関連抗体

Cell Viability Assay[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.
体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice
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.
分子量

469.84

分子式

C22H19ClF3NO5
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1284 mL 10.6419 mL 21.2838 mL
5 mM 0.4257 mL 2.1284 mL 4.2568 mL
10 mM 0.2128 mL 1.0642 mL 2.1284 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

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純度とドキュメンテーション

純度: 99.76%

COA (251 KB) RP-HPLC (222 KB) MS (68 KB)

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
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Voruciclib Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Voruciclib1000023-04-0CDKCyclin dependent kinaseclinicalstageorallyCDK9MCL-1multiplemodelsdiffuselargeB-celllymphomaDLBCLInhibitorinhibitorinhibit

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製品名:
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製品番号:
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