MSC-4106 - ≥99% , CAS No.2738542-58-8

CAS: 2738542-58-8 Cat. No.: M647720 分子式: C₁₈H₁₂F₃N₃O₂ 分子量: 359.30

GRADE & PURITY ≥99%

Storage

Store at -20°C,Desiccated

Shipped In

Ice chest + Ice pads

概要

MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD . MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model

In Vitro

MSC-4106 (10 μM, 24 h) inhibited SK-HEP-1 reporter and NCI-266 cell viability with IC 50 values of 4 nM and 14 nM, respectively. MSC-4106 (10 μM, 6 h) crystallizes in the P-site of TEAD1, and against TEAD1 or TEAD3 palmitoylation in TEAD-Overexpressing HEK293 Cells by 97.3% and 75.9%, respectively. MSC-4106 (10 μM, 4 d) targets TEAD indicated by a reduction in viability of NCI-H226 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: NCI-H226 (YAP dependent); SW620 YAP/TAZ KO (Yap-independent) cells Concentration: 0, 3, 6, 9, 12, 15, 18, 21, 24, 26, 30 μM Incubation Time: 96 hours Result: Showed inhibitory effect to NCI-H226 and general cytotoxic to SW620 (IC 50 >30 μM). ImmunofluorescenceCell Line: SK-HEP-1 Concentration: 0, 3, 6, 9, 12, 15, 18, 21, 24, 26, 30 μM Incubation Time: 24 hours Result: Inhibited YAP-TEAD interation.

In Vivo

MSC-4106 (100 mg/kg/d; p.o.; 7 d) displays anti-tumor effect with controlled tumor volume and good tolerability with stable body weight in mice . MSC-4106 (1, 5, 100 mg/kg/d; p.o.; 0-72 h) down-regulates Cyr61 (cysteine-rich angiogenic inducer 61) expression, the TEAD-regulated target gene, in tumor lysates at all time points at 100 mg/kg and 24 h at 5 mg/kg . Pharmacokinetics (PK) profile in different species Parameter Mouse Rat Dog Cl (l/h/kg) 0.2 0.7 0.05 PO t 1/2 (h) 45 40 3.6 PO AUC (μg•h/mL) 45 10 33 V ss (L/kg) 2 5 0.3 F (%) >90 80 18 Note : PO studies were performed at 10 mg/kg ; MSC-4106 was formulated in 20% Kleptose in 50 mM PBS at pH 7.4. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NCI-H226 xenograft model in H2d Rag2 female mice (9-week-old) Dosage: 5, 100 mg/kg Administration: Oral gavage; once daily; 32 days Result: Resulted tumor growth controlled with 5 mg/kg while regressed with 100 mg/kg dosing after 32 treatment days.

Form:Solid

IC50& Target:Target: YAP

Specifications

仕様と純度

≥99%

生化学的・生理学的メカニズム

MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD . MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model.

保管条件

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: 359.30

化学的性質と物理的性質

• 溶解度: DMSO : 250 mg/mL (695.80 mM; Need ultrasonic)

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, 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 2738542-58-8, the molecular formula is C18H12F3N3O2, and the molecular weight is 359.30 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.