ChemicalBook > CAS DataBase List > MI-463

MI-463

Product Name: MI-463
CAS No.: 1628317-18-9
Chemical Name: MI-463
Synonyms: MI-463, 10 mM in DMSO;MI-463;MI 463;MI463;1628317-18-9;MI463,Epigenetic Reader Domain,MI-463,MI 463,Inhibitor,inhibit;4-Methyl-5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)meth;4-Methyl-5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile;1H-Indole-2-carbonitrile, 4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-
CBNumber: CB63154812
Molecular Formula: C24H23F3N6S
Formula Weight: 484.54
MOL File: 1628317-18-9.mol

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MI-463 Property

Boiling point:: 663.2±55.0 °C(Predicted)
Density: 1.43±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: soluble; Ethanol: soluble
form: A crystalline solid
pka: 14.56±0.30(Predicted)
color: White to light yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-6219
Product name: MI-463
Purity: 99.57%
Packaging: 1mg
Price: $84
Updated: 2021/12/16

ChemScene

Product number: CS-6219
Product name: MI-463
Purity: 99.57%
Packaging: 5mg
Price: $180
Updated: 2021/12/16

ChemScene

Product number: CS-6219
Product name: MI-463
Purity: 99.57%
Packaging: 10mg
Price: $252
Updated: 2021/12/16

ChemScene

Product number: CS-6219
Product name: MI-463
Purity: 99.57%
Packaging: 100mg
Price: $804
Updated: 2021/12/16

ChemScene

Product number: CS-6219
Product name: MI-463
Purity: 99.57%
Packaging: 50mg
Price: $564
Updated: 2021/12/16

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MI-463 Chemical Properties,Usage,Production

Uses

MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

Biological Activity

MI-463 is a potent inhibitor of Menin-MLL interaction with IC50 of 15.3 nM.

in vivo

MI-463 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (45%). Pharmacologic inhibition of the menin-mLL interaction substantially delays progression of mLL leukemia in murine models through on-target activity without causing toxicity. MI-463 induces strong inhibition of tumor growth with once daily intraperitoneal (i.p.) administration. The expression of mLL fusion protein target genes, HOXA9 and MEIS1, are significant reduced upon treatment with MI-463. 20 days treatment of MV4;11 xenograft recipient mice with MI-463 also results in a substantial delay in leukemia progression as manifested by a marked decrease in the bioluminescence level which is associated with a significant decrease in the population of leukemic cells in the peripheral blood, spleen and bone marrow samples^[1].

target

Target	Value
Menin-MLL interaction (Cell-free assay)	15.3 nM

References

[1] Borkin D, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell. 2015 Apr 13;27(4):589-602. DOI:10.1016/j.ccell.2015.02.016

MI-463 Preparation Products And Raw materials

Raw materials

Preparation Products

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1628317-18-9, MI-463Related Search:

D18

4-Methyl-5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)meth

MI-463;MI 463;MI463;1628317-18-9

1H-Indole-2-carbonitrile, 4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-

MI463,Epigenetic Reader Domain,MI-463,MI 463,Inhibitor,inhibit

4-Methyl-5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile

MI-463, 10 mM in DMSO

1628317-18-9

C24H23F3N6S