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 ≥ 5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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Senexin B is a potent, orally active CDK8/19 inhibitor with Kd values of 140 nM and 80 nM for CDK8 and CDK19, respectively. |
| Q901
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