M-1211 - ≥99% , CAS No.2377337-93-2

CAS: 2377337-93-2 Cat. No.: M649123 分子式: C₄₂H₅₇FN₆O₆S 分子量: 793.00

GRADE & PURITY ≥99%

Storage

Protected from light,Store at -20°C,Desiccated

Shipped In

Ice chest + Ice pads

概要

M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression

In Vitro

M-1121 (0~100 nM; 24 hours; MV4;11 cells) drives dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line. M-1121 establishes covalent interactions with Cysteine 329 located in the MLL binding pocket of menin and potently inhibits growth of acute leukemia cell lines carrying MLL translocations with no activity in cell lines with wild-type MLL. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell Line: MV4;11 cells Concentration: 0~100 nM Incubation Time: 24 hours Result: Drived dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line.

In Vivo

M-1121 (100 mg/kg; p.o.; 26 days) reduces the average tumor volume from 157 mm 3 at the beginning of the treatment to 106 mm 3 on day 26 of the treatment, a reduction of tumor volume of 32% . M-1121 (300 mg/kg; p.o.) leads to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment . M-1121 (5 mg/kg; p.o.) has a low clearance and a moderate volume of distribution . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice Dosage: 100 mg/kg Administration: P.o. Result: Reduced the average tumor volume from 157 mm 3 at the beginning of the treatment to 106 mm 3 on day 26 of the treatment, a reduction of tumor volume of 32%. Animal Model: SCID mice Dosage: 300 mg/kg Administration: P.o. Result: Led to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment. Animal Model: Female C57BL/6 mice Dosage: 5 mg/kg (Pharmacokinetic Analysis) Administration: P.o. Result: Had a low clearance and a moderate volume of distribution.

Form:Solid

IC50& Target:menin-MLL interaction

Specifications

仕様と純度

≥99%

生化学的・生理学的メカニズム

M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.

保管条件

Protected from light,Store at -20°C,Desiccated

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

≥99%

名前と識別子

分子量

793.00

よくある質問

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C, protected from light, desiccated. Keep the container tightly closed with desiccant — the material is moisture-sensitive.

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 2377337-93-2, the molecular formula is C42H57FN6O6S, and the molecular weight is 793.00 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.