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RBN012759

Cat. No. M13391
RBN012759 Structure
Size Price Availability Quantity
5mg USD 380  USD380 In stock
10mg USD 650  USD650 In stock
25mg USD 1250  USD1250 In stock
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Quality Control & Documentation
Biological Activity

RBN012759 is a potent, selective and orally active PARP14 inhibitor with IC50 values of <3 nM and 5 nM against the human and mouse catalytic domains, respectively. AIDS in the anti-tumor immune response.

Chemical Information
Molecular Weight 378.46
Formula C19H23FN2O3S
CAS Number 2360851-29-0
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage 4°C, protect from light, dry, sealed
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] Ying Zhu, et al. Clin Immunol. PARP14 promotes the growth and glycolysis of acute myeloid leukemia cells by regulating HIF-1α expression

[2] Alex M Eddie, et al. Immunohorizons. Selective Pharmaceutical Inhibition of PARP14 Mitigates Allergen-Induced IgE and Mucus Overproduction in a Mouse Model of Pulmonary Allergic Response

[3] Laurie B Schenkel, et al. Cell Chem Biol. A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants

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  Catalog
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Keywords: RBN012759 supplier, PARP, inhibitors, activators


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