SR-5037
Based on 1 Customer Validation
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.58%
- CAS No.: 2387704-74-5
- 화학식: C21H18Cl2F2N10O
- 분자량:535.34
-
보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Kinase Inhibitor Library
HY-L009
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Orally Active Compound Library
HY-L061
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Blood Cancer Compound Library
HY-L079
-
Cancer Stem Cells Compound Library
HY-L135
-
Molecular Glue Compound Library
HY-L137
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Anti-Hematopathy Compound Library
HY-L171
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
High-Efficiency Gene Editing Compound Library
HY-L244
Biological Activity
|
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) |
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.
-
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.
-
Cell Line:MDA-MB-231 cells
-
Concentration:100 nM
-
Incubation Time:4 h
-
Result:Weakened the anticyclin K antibody
(red) signal，degraded CycK
-
Cell Line:MDA-MB-231 cells
-
Concentration:100 nM
-
Incubation Time:1, 2, 4 h
-
Result:Gradually reduced her CycK protein intake.
| 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 % |
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.
Chemical Information
-
CAS No. 2387704-74-5
-
Appearance Solid
-
분자량 535.34
-
화학식 C21H18Cl2F2N10O
-
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
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
-
Data Sheet (279 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
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 |
SR-5037 Related Classifications
HY-181405 Related Classifications
Powered by Bioz