1. Protein Tyrosine Kinase/RTK
  2. Ephrin Receptor
  3. Targefrin

Targefrin 是一种有效的靶向 EphA2 的试剂,作为拮抗剂发挥作用。Targefrin 结合 EphA2- LBD 的解离常数为 21 nM,IC50 值为10.8 nM。Targefrin 在几种胰腺癌细胞系中诱导细胞受体内化和降解。

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Custom Peptide Synthesis

Targefrin Chemical Structure

Targefrin Chemical Structure

CAS No. : 3031514-44-7

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
500 μg ¥2380
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1 mg ¥3800
In-stock
5 mg ¥9000
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50 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Targefrin is a potent EphA2-targeting agent, acts as an antagonist. Targefrin binds EphA2-LBD with 21 nM dissociation constant and an IC50 value of 10.8 nM. Targefrin induces cellular receptor internalization and degradation in several pancreatic cancer cell lines[1].

体外研究
(In Vitro)

Targefrin (0.025-10 μM; 20 min) effectively antagonizes EphA2 degradation in BxPC3 pancreatic cancer cells[1].
Targefrin (2-10 μM; 24 h) significantly inhibits pancreatic cancer cell BxPC3 migration[1].

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

Western Blot Analysis[1]

Cell Line: BxPC3 cells (starved for 1 h and pre-treated with Targefrin for 20 min, followed by a combination treatment with 2 μg/mL ephrinA1-Fc for 3 h)
Concentration: 0.025, 0.25, 0.5, 1, 2.5, 5, 7.5 and 10 μM
Incubation Time: 20 min
Result: Effectively antagonized EphA2 degradation induced by the potent ephrinA1-Fc ligand, with an approximate EC50 of ~1.6 μM.

Cell Migration Assay [1]

Cell Line: BxPC3 cells
Concentration: 2, 4, 5 and 10 μM
Incubation Time: 24 h
Result: Significantly inhibited pancreatic cancer cell migration.
体内研究
(In Vivo)

Targefrin (50 mg/kg; i.v.; for 5 days) suppresses tumor growth when conjugated with Paclitaxel[1].

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

Animal Model: Male nu/nu mice (injected with MIA PaCa-2 cells)[1]
Dosage: 50 mg/kg
Administration: i.v.; at day 1, 4, 8, 11 and 15
Result: Both Targefrin-Paclitaxel and Targefrin-dimer-Paclitaxel displayed a significant antitumor effect compared to both the untreated group and the Paclitaxel-treated group.
Animal Model: Balb/C mice[1]
Dosage: 50 mg/kg
Administration: IV via tail vein; single dosage
Result: Cmax ~650 ng/mL after 2 hours from the injection; estimated t1/2 ~15 hr.
分子量

1700.94

Formula

C85H116F3N19O15

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

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (58.79 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 0.5879 mL 2.9396 mL 5.8791 mL
5 mM 0.1176 mL 0.5879 mL 1.1758 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

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

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 0.5879 mL 2.9396 mL 5.8791 mL 14.6978 mL
5 mM 0.1176 mL 0.5879 mL 1.1758 mL 2.9396 mL
10 mM 0.0588 mL 0.2940 mL 0.5879 mL 1.4698 mL
15 mM 0.0392 mL 0.1960 mL 0.3919 mL 0.9799 mL
20 mM 0.0294 mL 0.1470 mL 0.2940 mL 0.7349 mL
25 mM 0.0235 mL 0.1176 mL 0.2352 mL 0.5879 mL
30 mM 0.0196 mL 0.0980 mL 0.1960 mL 0.4899 mL
40 mM 0.0147 mL 0.0735 mL 0.1470 mL 0.3674 mL
50 mM 0.0118 mL 0.0588 mL 0.1176 mL 0.2940 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.

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产品名称:
Targefrin
目录号:
HY-P3717
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