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VTP50469

Cat. No. M13341
VTP50469 Structure
Size Price Availability Quantity
10mg USD 560  USD560 In stock
25mg USD 900  USD900 In stock
50mg USD 1200  USD1200 In stock
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Quality Control & Documentation
Biological Activity

VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL Interaction with a Ki value of 104 pM. VTP50469 has anti-leukemia activity.

Chemical Information
Molecular Weight 630.82
Formula C32H47FN6O4S
CAS Number 2169916-18-9
Solubility (25°C) DMSO ≥ 60 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] Derek H Janssens, et al. Nat Genet. Automated CUT&Tag profiling of chromatin heterogeneity in mixed-lineage leukemia

[2] Emily B Heikamp, et al. Blood. The menin-MLL1 interaction is a molecular dependency in NUP98-rearranged AML

[3] Michael C Gundry, et al. Cancer Cell. It's All About MEis: Menin-MLL Inhibition Eradicates NPM1-Mutated and MLL-Rearranged Acute Leukemias in Mice

[4] Hannah J Uckelmann, et al. Science. Therapeutic targeting of preleukemia cells in a mouse model of NPM1 mutant acute myeloid leukemia

[5] Andrei V Krivtsov, et al. Cancer Cell. A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia

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  Catalog
Abmole Inhibitor Catalog




Keywords: VTP50469 supplier, Histone Methyltransferase, inhibitors, activators


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