2. Cell Cycle/DNA Damage
  3. CDK
  4. SHR5428

SHR5428 是一种口服有效，选择性非共价 CDK7 抑制剂，具有高效的 CDK7 酶活性 (IC50=2.3 nM)。SHR5428 抑制 MDA-MB-468 细胞上的三阴性乳腺癌细胞活性 (IC50=6.6 nM)。

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SHR5428 Chemical Structure

SHR5428 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
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100 mg   询价  
250 mg   询价  

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Customer Review

SHR5428 相关抗体

Top Publications Citing Use of Products

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

SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM)[1].

IC50 & Target

CDK7

0.005 μM (IC50)

CDK12

1.11 μM (IC50)

CDK4

3.87 μM (IC50)

CDK6

5.89 μM (IC50)

CDK9

8.30 μM (IC50)

CDK2

8.99 μM (IC50)

CDK1

>100 μM (IC50)

体内研究
(In Vivo)

SHR5428（3-30 mg/kg，口服，每天一次，持续 21 天）显示出剂量依赖性肿瘤生长抑制[1]。
SHR5428（2 mg/kg，口服，一次）在小鼠、大鼠和狗等不同物种中表现出良好的药代动力学特性[1]。
Pharmacokinetic Parameters of SHR5428 in mouse, rat and dog[1].

Mouse (2 mg/kg) Rat (2 mg/kg) Dog (2 mg/kg)
Cmax (ng/mL) 116 120 543
AUC (ng/mL∗h) 139 556 4101
t1/2 (h) 0.7 2.6 4.9
Bioavailability F% 32% 44%
92%

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

Animal Model: HCC70 cell line derived xenograft NDG mouse model[1]
Dosage: 3, 10, 30 mg/kg
Administration: PO, once a day for 21 days
Result: Showed dose-dependent tumor growth inhibition (3 mg/kg, TGI = 39%; 10 mg/kg, TGI = 61%; 30 mg/kg, TGI = 83%).
分子量

477.42

Formula

C22H23F3N5O2P
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

SHR5428 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:

SHR5428SHR 5428SHR-5428CDKCyclin dependent kinaseMDA-MB-468orally activeInhibitorinhibitorinhibit

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Inquiry Information

产品名称：
SHR5428
目录号：
HY-155787
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