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 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 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|
|Administration||PO 5 days per week|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 5 mg/mL|
|Related CDK Products|
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Zotiraciclib (TG02, SB1317) is an orally bioavailable, brain penetrant multi-kinase inhibitor of CDK2, JAK2, and FLT3 with IC50 values of 13, 73, and 56 nM, respectively.
Trilaciclib (G1T28) is a potent first-in-class reversible CDK4/6 inhibitor with IC50 of 1 nM and 4 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.
CDKI-73 is a potent and orally active CDK9 inhibitor with Ki of 4 nM.
THZ531 is a covalent CDK12 and CDK13 inhibitor with IC50 values of 158 nM and 69 nM, respectively.
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