2. PROTAC Cell Cycle/DNA Damage
  3. Molecular Glues CDK
  4. SR-5037

SR-5037 是一种具有口服活性的 CDK12 (IC50 = 31 nM)/CDK13 抑制剂及 CycK (DC50 = 30 nM;
Dmax > 98%) 分子胶降解剂。SR-5037 可抑制 CDK12/CycK 和 CDK13/CycK 复合物的酶活性。SR-5037 可促进 DDB1 募集至 CDK12/CycK 复合物，进而触发蛋白酶体介导的 CycK 降解。SR-5037 在三阴性乳腺癌小鼠中可降解 CycK 活性。SR-5037 可用于三阴性乳腺癌等癌症的研究。

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SR-5037

SR-5037 Chemical Structure

CAS No. : 2387704-74-5

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SR-5037 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 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-5037 is an orally active CDK12 (IC50 = 31 nM)/CDK13 inhibitor and CycK (DC50 = 30 nM;
Dmax > 98%) molecular glue degrader. SR-5037 inhibits the enzymatic activity of CDK12/CycK and CDK13/CycK complexes. SR-5037 promotes the recruitment of DDB1 to the CDK12/CycK complex, thereby triggering proteasome-mediated CycK degradation. SR-5037 degrades active CycK in mouse models of triple-negative breast cancer. SR-5037 can be used in the research of cancers such as triple-negative breast cancer[1].

IC50 & Target[1]

CDK12

31 nM (IC50)

CDK13

 

CDK12/Cyclin K

58.7 nM (IC50)

CDK13/Cyclin K

234.6 nM (IC50)

CDK12/Cyclin K

139 nM (Kd)

体外研究
(In Vitro)

SR-5037 (1μM) 抑制 WEE1 (59.8%)、mTOR (50.6%) 和 CDK15 (49.2%) 激酶活性[1]。
SR-5037 (0.000001-10 μM; 2 h (room temperature)) 抑制纯化的人源 CDK12/CycK (IC50 = 58.7 nM，Kd = 139 nM) 和 CDK13/CycK (IC50 = 134.6 nM) 复合物的酶活性，促进 CDK12/CycK 与 DDB1形成了稳定的三元复合物 (Kd = 2.81 nM)[1]。
SR-5037 (100 nM, 1-4 h) 在 MDA-MB-231 细胞中诱导 CycK 发生强效且快速的降解[1]。
SR-5037 (2 h) 在 HiBiT-CycK 敲入型 A549 细胞中降解 cyclin K，DC50 为 30 nM，Dmax > 95%[1]。

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

SR-5037 相关抗体:

Cell Viability Assay[1]

Cell Line: MDA-MB-231 human triple-negative breast cancer cells
Concentration: 0.000000037-10 μM
Incubation Time: 72 h
Result: Inhibited MDA-MB-231 cell proliferation with a half-maximal growth inhibition concentration (GI50) of 9 nM.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells
Concentration: 100 nM
Incubation Time: 4 h
Result: Weakened the anticyclin K antibody
(red) signal，degraded CycK

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 100 nM
Incubation Time: 1, 2, 4 h
Result: Gradually reduced her CycK protein intake.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC0-t T1/2 F
Mice[1] 20 mg/kg p.o. 6.52 μM 30.2 μM·h 6.52 h 13 %
体内研究
(In Vivo)

SR-5037 (2-18 mg/kg; p.o.; single dose) 可在 NSG 小鼠的三阴性乳腺癌肿瘤中诱导呈剂量依赖性的 CycK 耗竭[1]。

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

Animal Model: NSG mice (female, nonirradiated, orthotopic triple-negative breast cancer model)[1]
Dosage: 2, 6, 18 mg/kg
Administration: p.o.; single dose
Result: Dose-dependently reduced CycK protein.
分子量

535.34

Formula

C21H18Cl2F2N10O
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-5037 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-50372387704-74-5SR5037SR 5037Molecular GluesCDKCyclin dependent kinaseCDK12/CDK13 InhibitorCycK Molecular Glue Degradermousetriple-negative breast cancerMDA-MB-231 cellsA549 cells
Inhibitorinhibitorinhibit

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