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SR-4835 is a highly selective, dual inhibitor of CDK12 and CDK13 with IC50 values of 99 nM, Kd of 98 nM and Kd of 4.9 nM, respectively. SR-4835 has potent in vivo anti-TNBC activity and augments the anti-cancer activity of cisplatin, irinotecan, and olaparib, which are standard-of-care therapeutics for TNBC.
| Cell Experiment | |
|---|---|
| Cell lines | MDA-MB-231, MDA-MB-436, HS578T, MDA-MB-468, FHC |
| Preparation method | Clonogenic Assays. 500 cells per well are plated in six-well dishes in triplicate. After overnight incubation, SR-4835 is added to the medium for 72 hr, and cells are allowed to grow for 7 to 10 days, during which medium is changed every 2 to 3 days. |
| Concentrations | 10-90 nM, 0.4-10 μM |
| Incubation time | 4 h, 6 h, 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Female SCID Beige mice bearing xenograft models BCM-4013 and BCM-3887 |
| Formulation | prepared in 10/90 DMSO/30% Hydroxypropyl-β-Cyclodextrin (hp-BCD) in water |
| Dosages | 20 mg/kg |
| Administration | PO 5 days per week |
| Molecular Weight | 499.36 |
| Formula | C21H20Cl2N10O |
| CAS Number | 2387704-62-1 |
| Solubility (25°C) | DMSO ≥ 6 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CDK Products |
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AT7519 is a novel small molecule multi-cyclin-dependent (CDK) kinase inhibitor. |
| Flavopiridol
Flavopiridol (Alvocidib) is a competitive broad-spectrum CDK inhibitor with IC50 of 30,170,100 nM against CDK1, CDK2 and CDK4, respectively. |
| R547
R547 is a potent and selective ATP-competitive CDK inhibitor, with Ki values of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively. |
| JNJ-7706621
JNJ-7706621 is a dual cell cycle inhibitor with activity against cyclin-dependent kinases (CDK1, 2, 3, 6) with an IC50 of 3-175 nM and Aurora kinases (A and B) with an IC50 of 11-15 nM respectively. |
| PD 0332991 HCL
PD-0332991 HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. |
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