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TH287

Cat. No. M13654
TH287 Structure
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Biological Activity

TH287 is a potent and selective inhibitor of MTH1, with an IC50 of 0.8 nM. TH287 is highly selective towards MTH1, with no relevant inhibition of MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase and ITPA at 100 μM. TH287 could act as a chemotherapeutic agent for cancer research.

Chemical Information
Molecular Weight 269.13
CAS Number 1609960-30-6
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] Huaping Chen, et al. Int J Mol Sci. Radiolabeled 6-(2, 3-Dichlorophenyl)-N4-methylpyrimidine-2, 4-diamine (TH287): A Potential Radiotracer for Measuring and Imaging MTH1

[2] Dankai Zhan, et al. Cancer Biother Radiopharm. MTH1 Inhibitor TH287 Suppresses Gastric Cancer Development Through the Regulation of PI3K/AKT Signaling

[3] Xiao-Lei Shi, et al. Colloids Surf B Biointerfaces. Delivery of MTH1 inhibitor (TH287) and MDR1 siRNA via hyaluronic acid-based mesoporous silica nanoparticles for oral cancers treatment

[4] Mian Wang, et al. Sci Rep. Understanding the molecular mechanism for the differential inhibitory activities of compounds against MTH1

[5] Aljona Saleh, et al. J Pharm Biomed Anal. Development and validation of method for TH588 and TH287, potent MTH1 inhibitors and new anti-cancer agents, for pharmacokinetic studies in mice plasma

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