MI-538

Modify Date: 2024-01-02 10:54:26

MI-538 structure	Common Name	MI-538
	CAS Number	1857417-10-7	Molecular Weight	566.6
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₇H₂₅F₃N₈OS	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of MI-538

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.

Name	MI-538

Description	MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.
Related Catalog	Signaling Pathways >> Epigenetics >> Histone Methyltransferase Research Areas >> Cancer
Target	IC50 : 21 nM (menin and MLL interaction); Kd: 6.5 nM (menin)[1]
In Vitro	MI-538 inhibits the proliferation of MLL leukemia cells with a GI50 of 83 nM. MI-538 shows no effect (up to 6 μM) on growth of the control cell lines HL-60 and HM-2, which do not harbor MLL translocations, demonstrating good selectivity toward MLL fusion protein transformed cells. MI-538 binds to menin with low nanomolar affinity (Kd=6.5 nM). Its potent cellular activity originates from the improved binding affinity to menin and possibly increased cell membrane permeability. Treatment with MI-538 results in strong down regulation of expression of Hoxa9 and Meis1 genes. About 100 nM 27 was sufficient to reduce by ~50% Hoxa9 expression in MLL-AF9 cells, and even more pronounced effect was seen on Meis1 expression[1].
In Vivo	Treatment with MI-538 results in a pronounced, about 80%, reduction in the MV4;11 tumor volume, without causing substantial signs of toxicity reflected by less than 10% reduction of the body weight. MI-538 demonstrates markedly improved exposure (area under the curve, AUC, values), Cmax (maximum compound concentration) in the blood plasma, and the lowest value of clearance. The half-life of MI-538 is about 1.6 h. MI-538 has also high oral bioavailability (~50%)[1].
Cell Assay	MOLM-13, MV4;11, HL-60 human leukemia cells as well as MLL-AF9 and HM-2 murine bone marrow cells are treated with MI-538 or 0.25% DMSO for 7 days. Media are changed at day 4 with viable cell number restored to the original concentration, and MI-538 are resupplied. An amount of 100 μL of cell suspension is transferred to 96-well plates for each sample in quadruplicates. Cell viability is measured using the MTT assay. Plates are read for absorbance at 570 nm[1].
Animal Admin	Mice: Mice xenograft are randomly grouped with each group containing eight mice. Vehicle or MI-538 (45 mg/kg) are administrated once daily at designated doses using ip injections for 2 weeks. Body weight and tumor sizes are monitored three times a week[1].
References	[1]. Borkin D, 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. 2016 Feb 11;59(3):892-913.

Molecular Formula	C₂₇H₂₅F₃N₈OS
Molecular Weight	566.6
Storage condition	2-8℃

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: MI-538
Price: Negotiable
Purity: 98.0%
Delivery: 10 Day
Contact: Huang
Email: sales@echemcloud.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: MI-538
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

DC Chemicals Limited
China
Product Name: MI-538
Price: $650.0/100mg $1200.0/250mg $2500.0/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

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Price: $359/10mM*1mLinDMSO

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