1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. JS25

JS25 是一种选择性的 BTK 共价抑制剂 (IC50=5.8 nM),通过螯合 Tyr551 而使 BTK 失活。JS25 抑制癌细胞增殖,诱导细胞死亡,对鼠中的 Burkitt 淋巴瘤异种移植模型具有改善效果。JS25 能够透过血脑屏障。

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JS25 Chemical Structure

JS25 Chemical Structure

CAS No. : 2411771-95-2

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
1 mg ¥1600
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5 mg ¥4200
In-stock
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC50 value of 5.8 nM by chelating Tyr551. JS25 inhibits cancer cells proliferation, pronounces cell death, and promotes murine xenograft model of Burkitt’s lymphoma. JS25 effectively crosses the blood-brain barrier[1].

IC50 & Target

IC50: 5.8 nM (BTK), 49.0 nM (BMX), 440 nM (ITK), 190 nM (TXK), 220 nM (TEC), 2.60 μM (BLK)[1]

体外研究
(In Vitro)

JS25 (0-50 μM; 72 h) inhibits the proliferation of myeloid and lymphoid B-cell cancer cell lines. JS25 shows inhibitory capability against BTK, BMX, ITK, TXK, TEC, and BLK with IC50s of 28.5 nM, 49.0 nM, 0.44 μM, 0.19 μM, 0.22 μM, and 2.60 μM, respectively; shows little inhibition against other BTK pathway-related proteins (EGFR, ERBB2, and JAK3), with IC50>3 μM. JS25 presents a more favorable selectivity profile than Ibrutinib (HY-10997) and Acalabrutinib (HY-17600)[1].
JS25 (10 μM; 0, 4, 15 h) degrades BTK and inhibits both the catalytic activity and the expression of BTK in tumor cells[1].
JS25 (10 μM; 72 h) inhibits the tumor growth of Burkitt’s lymphoma and induces selective ex vivo cytotoxicity in primary diffuse large B-cell lymphoma (DLBCL) samples[1].

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

体内研究
(In Vivo)

JS25 (10 mg/kg and 20 mg/kg; i.p.; every 2 days, for 14 d) inhibits tumor growth and results a significant reduction in their secondary tumor formation in murine xenograft model of Burkitt’s lymphoma[1].
JS25 (1, 2.5, and 5 μM; injection; every day for 2 days) decreases tumor burden in zebrafish patient-derived xenografts of chronic lymphocytic leukemia, wich efficacy is better than Ibrutinib (HY-10997)[1].

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

Animal Model: Female adult BALB/c/NSG mice with Raji cells (s.c.)[1]
Dosage: 10 mg/kg and 20 mg/kg
Administration: Intraperitoneal injection; every 2 days for 14 days
Result: Caused a 30-40% reduction of the subcutaneous tumor and an overall reduction in the percentage of metastasis and secondary tumor formation.
分子量

524.59

Formula

C29H24N4O4S

CAS 号
性状

固体

颜色

Light yellow to light brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°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 : 20 mg/mL (38.13 mM; 超声助溶 (<60°C); 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 1.9063 mL 9.5313 mL 19.0625 mL
5 mM 0.3813 mL 1.9063 mL 3.8125 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 1.9063 mL 9.5313 mL 19.0625 mL 47.6563 mL
5 mM 0.3813 mL 1.9063 mL 3.8125 mL 9.5313 mL
10 mM 0.1906 mL 0.9531 mL 1.9063 mL 4.7656 mL
15 mM 0.1271 mL 0.6354 mL 1.2708 mL 3.1771 mL
20 mM 0.0953 mL 0.4766 mL 0.9531 mL 2.3828 mL
25 mM 0.0763 mL 0.3813 mL 0.7625 mL 1.9063 mL
30 mM 0.0635 mL 0.3177 mL 0.6354 mL 1.5885 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:
JS25
目录号:
HY-151808
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