An inhibitor of menin-MLL fusion protein interactions

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Product Categories

Product Type

Biochemicals

Research Area

Cancer

MI-463

Name: MI-463
Brand: -

Item No. 33525

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)

Technical Information

Formal Name

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

CAS Number

1628317-18-9

Molecular Formula

C₂₄H₂₃F₃N₆S

Formula Weight

484.5

Purity

≥98%

Formulation (Request formulation change)

A crystalline solid

Solubility(Learn about Variance in Solubility)

DMSO: SolubleEthanol: Soluble

λ_max

226, 230, 279, 287 nm

SMILES

N#CC1=CC2=C(C)C(CN3CCC(CC3)NC4=C5C=C(CC(F)(F)F)SC5=NC=N4)=CC=C2N1

InChi Code

InChI=1S/C24H23F3N6S/c1-14-15(2-3-21-19(14)8-17(11-28)31-21)12-33-6-4-16(5-7-33)32-22-20-9-18(10-24(25,26)27)34-23(20)30-13-29-22/h2-3,8-9,13,16,31H,4-7,10,12H2,1H3,(H,29,30,32)

InChi Key

DZACSLYTXLZAAF-UHFFFAOYSA-N

Shipping & Storage Information

Storage

-20°C

Shipping

Room temperature in continental US; may vary elsewhere

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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1 mg

$36

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5 mg

$110

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10 mg

$203

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25 mg

$378

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Product Description

MI-463 is an inhibitor of the protein-protein interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC₅₀ = 15 nM).¹ It inhibits growth of mouse bone marrow cells (BMCs) expressing the MLL fusion protein MLL-AF9 (GI₅₀ = 0.23 µM), as well induces differentiation of MLL-AF9-transformed BMCs.² MI-463 (0.75-6 µM) reduces colony formation by patient-derived acute myeloid leukemia (AML) cells. It reduces tumor growth in an MV4-11 mouse xenograft model when administered at a dose of 35 mg/kg.

WARNING This product is not for human or veterinary use.

References & Product Citations

Product Description References

1. Borkin, D., Pollock, J., Kempinska, K., et al. Property focused structure-based optimization of small molecule inhibitors of the protein-protein interaction between menin and mixed lineage leukemia (MLL). J. Med. Chem. 59(3), 892-913 (2016).

2. Borkin, D., He, S., Miao, H., et al. Pharmacologic inhibition of the menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell 27(4), 589-602 (2015).

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