2. Cell Cycle/DNA Damage
  3. CDK
  4. PROTAC CDK12/13 Degrader-1

PROTAC CDK12/13 Degrader-1 (7f) 是一种高效选择性的细胞周期蛋白依赖性激酶 CDK12/CDK13 双重降解剂，其 DC50 值分别是 2.2 nM 和 2.1 nM。PROTAC CDK12/13 Degrader-1 具有抗增殖活性，可用于乳腺癌的研究。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 PROTAC CDK12/13 Degrader-1 TFA 通常具有更好的水溶性和稳定性。

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PROTAC CDK12/13 Degrader-1 Chemical Structure

PROTAC CDK12/13 Degrader-1 Chemical Structure

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规格 价格 是否有货
1 mg ￥3500
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5 mg ￥8500
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PROTAC CDK12/13 Degrader-1 的其他形式现货产品:

Customer Review

Other Forms of PROTAC CDK12/13 Degrader-1:

PROTAC CDK12/13 Degrader-1 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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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

PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research[1].

IC50 & Target[1]

CDK12

2.2 nM (DC50)

CDK13

2.1 nM (DC50)

体外研究
(In Vitro)

PROTAC CDK12/13 Degrader-1 (0.02-10 μM, 150 h) 显著并呈呈剂量依赖性抑制 MFM223 和 MDA-MB-231 细胞的增殖[1]。
PROTAC CDK12/13 Degrader-1 (500 nM, 4 h) 以剂量依赖性方式显著降解 MFM223 和 MDA-MB-231 细胞的 CDK12 和 CDK13[1]。

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

PROTAC CDK12/13 Degrader-1 相关抗体:

Immunofluorescence[1]

Cell Line: MDA-MB-231 cell lines
Concentration: 1.0 μM
Incubation Time: 15 hours
Result: Showed 88% degradation for CDK12 and 74% for CDK13.
Acted on CDK12 with the DC50 value of 2.2 nM, and acted on CDK13 with the DC50 value of 2.1 nM.
体内研究
(In Vivo)

The pharmacokinetic parameters of PROTAC CDK12/13 Degrader-1 (7f) in rats[1].

Parameters oral (20 mg/kg) iv (10 mg/kg) ip (20 mg/kg) iv (2.5 mg/kg)
t1/2 (h) - 5.28 10.85 5.8
Tmax (h) 5.33 0.08 2.17 0.08
Cmax (ng/mL) 7.73 19892.4 24.79 1498.5
Cmax (ng/mL) 7.73 19892.4 24.79 1498.5
AUC0-t(h*ng/mL) 21.83 7193.3 284.8 383.9
AUC0-∞(h*ng/mL) - 7242.7 318.5 391.55
CL (mL/h/kg) - 1406.5 - 6495.4
F (%) 0.15 - 10.63 -

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

822.91

Formula

C45H46N10O6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PROTAC CDK12/13 Degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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:

PROTAC CDK12/13 Degrader-1CDKCyclin dependent kinaseCDK12CDK13PROTACanti-proliferativebreast cancerTNBCInhibitorinhibitorinhibit

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