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TTT 3002 

Cat. No. M30770
TTT 3002  Structure
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Biological Activity

TTT 3002 is a potent and orally active FLT3 inhibitor. TTT 3002 potently inhibits FLT3 phosphorylation by activating mutations at residue D835, with an IC50 of 0.2 nM. TTT 3002 can be used for AML (acute myeloid leukemia) research.

Chemical Information
Molecular Weight 465.5
Formula C27H23N5O3
CAS Number 871037-95-5
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Mei Wu, et al. J Hematol Oncol. FLT3 inhibitors in acute myeloid leukemia

[2] Hayley S Ma, et al. Cancer Res. FLT3 kinase inhibitor TTT-3002 overcomes both activating and drug resistance mutations in FLT3 in acute myeloid leukemia

[3] Hayley Ma, et al. Blood. TTT-3002 is a novel FLT3 tyrosine kinase inhibitor with activity against FLT3-associated leukemias in vitro and in vivo

[4] Chen Yao, et al. Hum Mol Genet. Kinase inhibitors arrest neurodegeneration in cell and C. elegans models of LRRK2 toxicity

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Keywords: TTT 3002  supplier, FLT3, inhibitors, activators


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