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RK-287107

Cat. No. M13713
RK-287107 Structure
Size Price Availability Quantity
5mg USD 240  USD240 In stock
10mg USD 360  USD360 In stock
50mg USD 1150  USD1150 In stock
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Quality Control & Documentation
Biological Activity

RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth.

Product Citations
Chemical Information
Molecular Weight 416.46
CAS Number 2171386-10-8
Solubility (25°C) DMSO 90 mg/mL
Storage 2-8°C, protect from light
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Fumiyuki Shirai, et al. J Med Chem. Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer

[2] Fumiyuki Shirai, et al. J Med Chem. Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase Inhibitors

[3] Anna Mizutani, et al. Cancer Sci. RK-287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model

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