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

Size Price Stock
5 mg Ask For Quote & Lead Time
10 mg Ask For Quote & Lead Time
25 mg Ask For Quote & Lead Time
50 mg Ask For Quote & Lead Time

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

SR-5037 Related Antibodies

Top Publications Citing Use of Products

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

SR-5037 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
SR-5037
Cat. No.:
HY-181405
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.