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MI-463

Cat. No. M9150
MI-463 Structure
Size Price Availability Quantity
5mg USD 180  USD180 In stock
10mg USD 280  USD280 In stock
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Quality Control & Documentation
Biological Activity

MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the Menin-MLL interaction, with an IC50 value of 15.3 nM. MI-463 is effective in inducing differentiation of MLL leukemia cells. Treatment with sub-micromolar concentrations of MI-463 also leads to markedly reduced expression of Hoxa9 and Meis1, downstream targets of MLL fusion proteins substantially upregulated in MLL leukemias.

In vivo, MI-463 induces strong inhibition of tumor growth with once daily intraperitoneal (i.p.) administration. In a mouse xenograft model using MV4;11 human MLL leukemia cells implanted into BALB/c nude mice, MI-463 induces strong inhibition of tumor growth with once-daily intraperitoneal (i.p.) administration. It does not impair normal hematopoiesis in vivo.

Chemical Information
Molecular Weight 484.54
Formula C24H23F3N6S
CAS Number 1628317-18-9
Solubility (25°C) DMSO: ≥ 85 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] Erzsbet Pszti-Gere, et al. In vitro interaction of potential antiviral TMPRSS2 inhibitors with human serum albumin and cytochrome P 450 isoenzymes

[2] Ichiroh Kato, et al. Menin‑MLL inhibitors induce ferroptosis and enhance the anti‑proliferative activity of auranofin in several types of cancer cells

[3] Jingyao Chen, et al. An organoid-based drug screening identified a menin-MLL inhibitor for endometrial cancer through regulating the HIF pathway

[4] Dmitry Borkin, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo

[5] Duk-Woo Park, et al. Impact of the angiographic mechanisms underlying periprocedural myocardial infarction after drug-eluting stent implantation

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Keywords: MI-463 supplier, Histone Methyltransferase, inhibitors, activators


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