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

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.

For research use only. We do not sell to patients.

SR-5037

SR-5037 Chemical Structure

CAS No. : 2387704-74-5

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SR-5037 Related Antibodies

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Description

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)

In Vitro

SR-5037 (1 μM) degrades CycK (DC50 = 30 nM;
Dmax > 98%) and inhibits the kinase activities of WEE1 (59.8%), mTOR (50.6%) and CDK15 (49.2%)[1].
SR-5037 (0.000001-10 μM; 2 h (room temperature)) inhibits the enzymatic activity of purified human CDK12/CycK (IC50 = 58.7 nM, Kd = 139 nM) and CDK13/CycK (IC50 = 134.6 nM) complexes, and promotes the formation of a stable ternary complex between CDK12/CycK and DDB1 (Kd = 2.81 nM)[1].
SR-5037 (100 nM, 1-4 h) potently and rapidly induces the degradation of CycK in MDA-MB-231 cells[1].
SR-5037 (2 h) degrades cyclin K in HiBiT-CycK knock-in A549 cells, with a DC50 of 30 nM and a Dmax > 95%[1].

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

SR-5037 Related Antibodies

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.
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 %
In Vivo

SR-5037 (2-18 mg/kg; p.o.; single dose) induces dose-dependent depletion of cyclin K in orthotopic triple-negative breast cancer tumors in female NSG mice, with target modulation correlating with plasma drug concentration[1].

MedChemExpress (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.
Molecular Weight

535.34

Formula

C21H18Cl2F2N10O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(C=C(N2)C(N=C2CNC3=C4C(N(C=N4)C(C=N5)=CN5C(F)F)=NC(N6CCOCC6)=N3)=C1)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 4.17 mg/mL (7.79 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8680 mL 9.3399 mL 18.6797 mL
5 mM 0.3736 mL 1.8680 mL 3.7359 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8680 mL 9.3399 mL 18.6797 mL 46.6993 mL
5 mM 0.3736 mL 1.8680 mL 3.7359 mL 9.3399 mL
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SR-5037 Related Classifications

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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