2. Cell Cycle/DNA Damage
  3. CDK
  4. KB-0742

KB-0742 是一种有效的，选择性的和具有口服活性的 CDK9 抑制剂，对 CDK9/cyclin T1 的 IC50 为 6 nM。KB-0742 对 CDK9/cyclin T1 具有选择性，其选择性是其他 CDK 激酶的 50 倍以上。KB-0742 具有有效的抗肿瘤活性。

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KB-0742 Chemical Structure

KB-0742 Chemical Structure

CAS No. : 2416873-83-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4214
In-stock
1 mg ￥1333
In-stock
5 mg ￥2600
In-stock
10 mg ￥4500
In-stock
25 mg 现货 询价
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100 mg   询价  

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Customer Review

Other Forms of KB-0742:

KB-0742 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity[1].

IC50 & Target[1]

CDK9/cyclinT1

6 nM (IC50)

体外研究
(In Vitro)

KB-0742 (6 hours; 0.1-10 μM; 22Rv1 cells) treatment significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5. Global androgen receptor (AR)-FL and AR-V protein levels are significantly reduced starting at 6 h treatment time, which is accompanied by the reduction of phospho-AR levels (Ser81)[1].
KB-0742 (48-72 hours) treatment shows cytostatic effects in prostate cancer and leukemia cell lines. KB-0742 shows antiproliferative activity with GR50s of 0.183 μM and 0.288 μM for 22Rv1 cells and MV-4-11 AML cells, respectively[1].
In 22Rv1 cells, KB-0742 rapidly downregulates nascent transcription, preferentially depleting short half-life transcripts and AR-driven oncogenic programs[1].

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

KB-0742 相关抗体:

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 10 μM
Incubation Time: 6 hours
Result: Significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5.
体内研究
(In Vivo)

KB-0742 (3-30 mg/kg; p.o.; daily; over 21 days) is well tolerated even at high dose, while significantly reducing tumor burden in 22Rv1 human prostate cancer cell line-derived xenograft (CDX) models[1].

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

Animal Model: Male CB17-SCID mice injected with 22Rv1 human prostate cancer cells[1]
Dosage: 3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration: p.o.; daily; over 21 days
Result: Significantly reduced tumor growth in castration-resistant prostate cancer (CRPC).
分子量

287.40

Formula

C16H25N5
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 175 mg/mL (608.91 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4795 mL 17.3974 mL 34.7947 mL
5 mM 0.6959 mL 3.4795 mL 6.9589 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.38%

COA (289 KB) HNMR (249 KB) LCMS (92 KB)

产品使用指南 (1538 KB)
参考文献

KB-0742 相关分类

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4795 mL 17.3974 mL 34.7947 mL 86.9868 mL
5 mM 0.6959 mL 3.4795 mL 6.9589 mL 17.3974 mL
10 mM 0.3479 mL 1.7397 mL 3.4795 mL 8.6987 mL
15 mM 0.2320 mL 1.1598 mL 2.3196 mL 5.7991 mL
20 mM 0.1740 mL 0.8699 mL 1.7397 mL 4.3493 mL
25 mM 0.1392 mL 0.6959 mL 1.3918 mL 3.4795 mL
30 mM 0.1160 mL 0.5799 mL 1.1598 mL 2.8996 mL
40 mM 0.0870 mL 0.4349 mL 0.8699 mL 2.1747 mL
50 mM 0.0696 mL 0.3479 mL 0.6959 mL 1.7397 mL
60 mM 0.0580 mL 0.2900 mL 0.5799 mL 1.4498 mL
80 mM 0.0435 mL 0.2175 mL 0.4349 mL 1.0873 mL
100 mM 0.0348 mL 0.1740 mL 0.3479 mL 0.8699 mL
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:

KB-07422416873-83-9KB0742KB 0742CDKCyclin dependent kinaseCDK9oralanticancerCRPCSer2Ser7Ser5antiproliferativeInhibitorinhibitorinhibit

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Inquiry Information

产品名称：
KB-0742
目录号：
HY-137478
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