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DT-061

Cat. No. M14489
DT-061 Structure
Size Price Availability
5mg USD 350  USD350 4-7 Days
10mg USD 550  USD550 4-7 Days
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Quality Control & Documentation
Biological Activity

DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.

Chemical Information
Molecular Weight 520.52
CAS Number 1809427-19-7
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Gianmatteo Vit, et al. Chemogenetic profiling reveals PP2A-independent cytotoxicity of proposed PP2A activators iHAP1 and DT-061

[2] Vidhi M Shah, et al. Select Stabilization of a Tumor-Suppressive PP2A Heterotrimer

[3] Garry L Coles, et al. Unbiased Proteomic Profiling Uncovers a Targetable GNAS/PKA/PP2A Axis in Small Cell Lung Cancer Stem Cells

[4] Daniel Leonard, et al. Selective PP2A Enhancement through Biased Heterotrimer Stabilization

[5] Otto Kauko, et al. PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells

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  Catalog
Abmole Inhibitor Catalog




Keywords: DT-061 supplier, Phosphatase, inhibitors, activators


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