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SR-4835

Cat. No. M10258
SR-4835 Structure
Synonym:

SR4835

Size Price Availability Quantity
5mg USD 351  USD390 In stock
10mg USD 585  USD650 In stock
25mg USD 999  USD1110 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 499.36
Formula C21H20Cl2N10O
CAS Number 2387704-62-1
Purity >98%
Solubility DMSO ≥ 5 mg/mL
Storage at -20°C
References

Induction of BRCAness in Triple-Negative Breast Cancer by a CDK12/13 Inhibitor Improves Chemotherapy
Jessica L Hopkins, et al. Cancer Cell. 2019 Nov 11;36(5):461-463. PMID: 31715127.

Therapeutic Targeting of CDK12/CDK13 in Triple-Negative Breast Cancer
Victor Quereda, et al. Cancer Cell. 2019 Nov 11;36(5):545-558.e7. PMID: 31668947.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SR-4835, SR4835 supplier, CDK, inhibitors

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