MI-3454 | menin-MLL1 inhibitor | Probechem Biochemicals

Chemical Structure : MI-3454

CAS No.: 2134169-43-8

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MI-3454 (MI 3454)

货号: PC-72046Not For Human Use, Lab Use Only.

MI-3454 (MI 3454) is a highly potent, orally bioavailable inhibitor of the menin-MLL1 interaction with IC50 of 0.51 nM, 60-fold improvement over MI-503.

规格	价格	库存
1 mg	￥1980	In stock
5 mg	￥4580	In stock
10 mg	￥7580	In stock
25 mg		Get quote
100 mg		Get quote

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生物&药学活性

MI-3454 (MI 3454) is a highly potent, orally bioavailable inhibitor of the menin-MLL1 interaction with IC50 of 0.51 nM, 60-fold improvement over MI-503.
MI-3454 inhibits growth of human MLL leukemic cell lines (MLL-tr): MV-4-11, MOLM-13, KOPN-8, SEM, RS4-11 with GI50 values of 7-27 nM in MTT cell viability assays, does not significantly (>100-fold) affect the growth of leukemic cells without MLL1 translocations.
MI-3454 (50 nM or lower) led to downregulated expression of HOXA9 and MEIS1 in MV-4-11 and MOLM13 cells, also reduced other MLL fusion target genes, including MEF2C, DLX2, HOXA10, PBX3, and FLT3.
MI-3454 demonstrated strong reduction of cell proliferation and downregulation of HOXA9 and MEIS1 expression in mouse bone marrow cells transformed with the MLL-AF9 oncogene but not in bone marrow cells transformed with HOXA9 and MEIS1 oncogenes.
MI-3454 induces leukemia regression in xenograft model of MLL leukemia through on-target activity.
MI-3454 (3–12 nM) substantially reduced clonogenic potential in MLL leukemia patient samples with MLL1 translocations or NPM1 mutations, MI-3454 induced complete remission or blocks leukemia progression in PDX models of MLL leukemia.

物理化学性质&存储条件

分子量	636.742
分子式	C32H35F3N8OS
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Formamide, N-[3-[[2-cyano-4-methyl-5-[[4-[[2-(methylamino)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-1H-indol-1-yl]methyl]bicyclo[1.1.1]pent-1-yl]-

参考文献

1. Klossowski S, et al. J Clin Invest. 2020 Feb 3;130(2):981-997.

2. Miao H, et al. Blood. 2020 Dec 17;136(25):2958-2963.

MI-3454 (MI 3454)

生物&药学活性

物理化学性质&存储条件

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MI-3454 (MI 3454)

生物&药学活性

物理化学性质&存储条件

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