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Chemical Structure| 2387704-62-1 Chemical Structure| 2387704-62-1

Structure of SR-4835
CAS No.: 2387704-62-1

Chemical Structure| 2387704-62-1

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SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 with IC50 of 99 nM, Kd of 98 nM for CDK12 and Kd of 4.9 nM for CDK13. It acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death.

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Product Details of SR-4835

CAS No. :2387704-62-1
Formula : C21H20Cl2N10O
M.W : 499.36
SMILES Code : CN1N=CC(N2C=NC3=C(NCC4=NC5=CC(Cl)=C(Cl)C=C5N4)N=C(N6CCOCC6)N=C23)=C1
MDL No. :MFCD32263441
InChI Key :FSELUFUYNUNZKD-UHFFFAOYSA-N
Pubchem ID :139600338

Safety of SR-4835

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of SR-4835

Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MDA-MB-231 cells 500 nM 1 hour SR-4835 promotes cyclin K degradation RSC Chem Biol. 2024 Oct 11;6(1):36–55
A549 cells 90 nM 2 hours SR-4835 effectively degrades cyclin K RSC Chem Biol. 2024 Oct 11;6(1):36–55
MDA-MB-468 9.21 nM (EC50) 120 hours Assessed anti-proliferative effect with EC50 of 9.21 nM Nat Commun. 2024 Aug 1;15(1):6477
MDA-MB-231 32.43 nM (EC50) 120 hours Assessed anti-proliferative effect with EC50 of 32.43 nM Nat Commun. 2024 Aug 1;15(1):6477
COLO829 1 µM 2 hours To assess the effect of SR-4835 on cyclin K levels, found that SR-4835 reduced cyclin K levels Cell Death Discov. 2023 Dec 16;9(1):459.
WM983B 1 µM 2 hours To assess the effect of SR-4835 on cyclin K levels, found that SR-4835 reduced cyclin K levels Cell Death Discov. 2023 Dec 16;9(1):459.
WM164 1 µM 2 hours To assess the effect of SR-4835 on cyclin K levels, found that SR-4835 reduced cyclin K levels Cell Death Discov. 2023 Dec 16;9(1):459.
A375 0.05, 0.1, 0.2, 0.5, 1 µM 2 hours To assess the effect of SR-4835 on cyclin K levels, found that SR-4835 reduced cyclin K levels in a dose-dependent manner Cell Death Discov. 2023 Dec 16;9(1):459.
Recombinant Cdk10/CycQ 0.2 µM 20 min To determine the inhibitory activity of SR-4835 against Cdk10/CycQ, IC50 value was 1070 nM. J Biol Chem. 2024 Jan;300(1):105501
SW620 100 nM 24 hours To evaluate the effect of SR-4835 on tumoursphere formation capacity, results showed that SR-4835 reduced the tumoursphere formation capacity of SW620 cells. Clin Transl Med. 2022 Oct;12(10):e1087
HCT116 100 nM 24 hours To evaluate the effect of SR-4835 on tumoursphere formation capacity, results showed that SR-4835 reduced the tumoursphere formation capacity of HCT116 cells. Clin Transl Med. 2022 Oct;12(10):e1087
SW620 100 nM 24 hours To evaluate the effect of SR-4835 on cell migration and invasion capacity, results showed that SR-4835 significantly reduced the migration and invasion capacity of SW620 cells. Clin Transl Med. 2022 Oct;12(10):e1087
HCT116 100 nM 24 hours To evaluate the effect of SR-4835 on cell migration and invasion capacity, results showed that SR-4835 significantly reduced the migration and invasion capacity of HCT116 cells. Clin Transl Med. 2022 Oct;12(10):e1087
Recombinant Cdk12/CycK 0.2 µM 60 min To determine the inhibitory activity of SR-4835 against Cdk12/CycK and Cdk13/CycK, IC50 values were 60 nM and 366 nM, respectively. J Biol Chem. 2024 Jan;300(1):105501

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Liver metastasis model Oral 20 mg/kg 5 days on, 2 days off per week for 3 weeks To evaluate the effect of SR-4835 on liver metastasis, results showed that SR-4835 significantly reduced the number and size of liver metastatic nodules. Clin Transl Med. 2022 Oct;12(10):e1087

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