SR-5037 |
Catalog No.GC80892
One-Click Copy Product Info
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SR-5037 is an orally active CDK12 ( IC50 = 31 nM)/ CDK13 inhibitor and CycK ( DC50 = 30 nM; D max > 98%) molecular glue degrader.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2387704-74-5
Sample solution is provided at 25 µL, 10mM.
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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].
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].
References:
[1]. Pandurangan T, et al. Structure-Activity and Structure-Degradation Relationship Studies of 2-Amino-6-(benzimidazol-2-ylmethyl)-N9-heteroarylpurines as Potent and Selective CDK12/13 Inhibitors and Cyclin K Degraders. J Med Chem. 2026 Feb 12;69(3):2287-2309.
| Cas No. | 2387704-74-5 | SDF | |
| Formula | C21H18Cl2F2N10O | M.Wt | 535.34 |
| Solubility | DMSO: 4.17 mg/mL (7.79 mM; ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.868 mL | 9.3399 mL | 18.6797 mL |
| 5 mM | 373.6 μL | 1.868 mL | 3.7359 mL |
| 10 mM | 186.8 μL | 934 μL | 1.868 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)