2. Cell Cycle/DNA Damage Stem Cell/Wnt Protein Tyrosine Kinase/RTK
  3. Casein Kinase FLT3 CDK
  4. SR-2890

SR-2890 是一种高选择性、ATP 竞争型的酪蛋白激酶 CK1δ 和 CK1ε 的抑制剂，IC50 分别为 4 nM 和 44 nM，对 CK1δ 的 Ki 为 14 nM，具有抗增殖效应。SR-2890 可阻断其丝氨酸/苏氨酸激酶活性，并弱抑制 FLT3、CDK4 等少数脱靶激酶，口服生物利用度为 10%，血脑屏障穿透率<1%。SR-2890 具有稳定的体外代谢和良好的体内药代动力学特性，有效抑制人 A375 黑色素瘤细胞生长。SR-2890 可用于黑色素瘤的研究，同时也是阿尔茨海默病等 CK1d/e 相关疾病的工具化合物。

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SR-2890

SR-2890 Chemical Structure

CAS No. : 1454584-91-8

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SR-2890 相关抗体

Top Publications Citing Use of Products

查看 Casein Kinase 亚型特异性产品:

查看所有亚型
CK1 CK2

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 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values ​​of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease[1].

IC50 & Target

CK1δ

4 nM (IC50)

CK1ε

44 nM (IC50)

Cdk4/cyclin D1

283 nM (IC50)

Cdk4/cyclin D3

368 nM (IC50)

CK1ε

14 nM (Ki)

体外研究
(In Vitro)

SR-2890 可抑制人 A375 黑色素瘤细胞的增殖 (EC50=38 nM) [1]。
SR-2890 具有人肝微粒体稳定性、溶解性，无 CYP 抑制活性 (T1/2=44 min；CYP 抑制活性 >10 μM) [1]。
SR-2890 对脱靶激酶 FLT3 (IC50=809 nM) 和 CDK4/细胞周期蛋白 D1 (IC50=283 nM)、CDK4/细胞周期蛋白 D3 (IC50=368 nM) 具有弱抑制作用 [1]。

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

SR-2890 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[1] 1 nM i.v. Cmax 4.6 μM
Mice[1] 1 nM i.v. CL 8.4 mL/min/kg
Mice[1] 1 nM i.v. AUC 4.16 μM·h
Mice[1] 1 nM i.v. T1/2 1.50 h
Mice[1] 1 nM i.v. F 10 %
分子量

477.92

Formula

C23H21ClFN9
CAS 号
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

SR-2890 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 *
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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)
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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:

SR-28901454584-91-8SR2890SR 2890Casein KinaseFLT3CDKCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Cyclin dependent kinaseCK1εhuman A375 melanoma cellsCYP inhibitionCDK4/cyclin D1solubilitycasein kinase 1εCK1δcasein kinase 1δhuman liver microsome stabilityhuman cancer cell linesATP-competitiveanimal xenograft studiescancer cellsmelanomaInhibitorinhibitorinhibit

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