MI-538 - ≥98% , CAS No.1857417-10-7

CAS: 1857417-10-7 Cat. No.: M651225 分子式: C₂₇H₂₅F₃N₈OS 分子量: 566.60

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

概要

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC 50 of 21 nM.

In Vitro

MI-538 inhibits the proliferation of MLL leukemia cells with a GI 50 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 (K d =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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%) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:IC50 : 21 nM (menin and MLL interaction),Kd: 6.5 nM (menin)

Specifications

仕様と純度

≥98%

生化学的・生理学的メカニズム

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC 50 of 21 nM.

保管条件

Store at -20°C

入荷

Ice chest + Ice pads

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

純度

≥98%

名前と識別子

• 分子量: 566.60

化学的性質と物理的性質

• 溶解度: DMSO : 100 mg/mL (176.49 mM; Need ultrasonic)

よくある質問

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1857417-10-7, the molecular formula is C27H25F3N8OS, and the molecular weight is 566.60 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.