MSC-4106|cas:2738542-58-8|西域试剂

MSC-4106,99.82%

产品编号：Bellancom-147208| CAS NO：2738542-58-8| 分子式：C₁₈H₁₂F₃N₃O₂| 分子量：359.30

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货号	价格	库存与货期
Bellancom-147208	￥3000.00	杭州北京（现货）
Bellancom-147208	￥4800.00	杭州北京（现货）
Bellancom-147208	￥9500.00	杭州北京（现货）
Bellancom-147208	￥14500.00	杭州北京（现货）

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MSC-4106

产品介绍

MSC-4106 是一种具有口服活性的 YAP/TAZ-TEAD 抑制剂。 MSC-4106 阻断 TEAD1 和 TEAD3 的 auto-palmitoylation，对 NCI-H226 异种移植瘤模型具有抑制作用。

生物活性

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.

体外研究

MSC-4106 (10 μM, 24 h) inhibited SK-HEP-1 reporter and NCI-266 cell viability with IC₅₀ 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell 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 (IC₅₀ >30 μM).

Immunofluorescence

Cell 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.

体内研究
(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.

西域 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.

体内研究

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.

西域 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.

体内研究

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.

西域 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.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7832 mL	13.9159 mL	27.8319 mL
5 mM	0.5566 mL	2.7832 mL	5.5664 mL
10 mM	0.2783 mL	1.3916 mL	2.7832 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献