2. Stem Cell/Wnt
  3. YAP
  4. MSC-4106

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。

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MSC-4106 Chemical Structure

MSC-4106 Chemical Structure

CAS No. : 2738542-58-8

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Customer Review

MSC-4106 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

Target: YAP[1]
体外研究
(In Vitro)

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[1].
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[1].
MSC-4106 (10 μM, 4 d) targets TEAD indicated by a reduction in viability of NCI-H226 cells[1].

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

MSC-4106 相关抗体:

Cell Viability Assay[1]

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[1]

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[1].
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[1].
Pharmacokinetics (PK) profile in different species[1]

Parameter Mouse Rat Dog
Cl (l/h/kg) 0.2 0.7 0.05
PO t1/2 (h) 45 40 3.6
PO AUC (μg•h/mL) 45 10 33
Vss (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)[1]
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.
分子量

359.30

Formula

C18H12F3N3O2
CAS 号
性状

固体

颜色

White to off-white

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)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 250 mg/mL (695.80 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

MSC-4106 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7832 mL 13.9159 mL 27.8319 mL 69.5797 mL
5 mM 0.5566 mL 2.7832 mL 5.5664 mL 13.9159 mL
10 mM 0.2783 mL 1.3916 mL 2.7832 mL 6.9580 mL
15 mM 0.1855 mL 0.9277 mL 1.8555 mL 4.6386 mL
20 mM 0.1392 mL 0.6958 mL 1.3916 mL 3.4790 mL
25 mM 0.1113 mL 0.5566 mL 1.1133 mL 2.7832 mL
30 mM 0.0928 mL 0.4639 mL 0.9277 mL 2.3193 mL
40 mM 0.0696 mL 0.3479 mL 0.6958 mL 1.7395 mL
50 mM 0.0557 mL 0.2783 mL 0.5566 mL 1.3916 mL
60 mM 0.0464 mL 0.2319 mL 0.4639 mL 1.1597 mL
80 mM 0.0348 mL 0.1739 mL 0.3479 mL 0.8697 mL
100 mM 0.0278 mL 0.1392 mL 0.2783 mL 0.6958 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MSC-41062738542-58-8MSC4106MSC 4106YAPYes-associated proteinorally activeHippo pathwayNCI-H226 cellsTEAD subtypepalmitoylationCyr61anti-tumorInhibitorinhibitorinhibit

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