1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. 2-(Bromomethyl)acrylic acid

2-(Bromomethyl)acrylic acid  (Synonyms: α-(Bromomethyl)acrylic acid; α-Methylated acrylamide; α-MAA)

目录号: HY-W017180
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2-(Bromomethyl) acrylic acid 是布鲁顿酪氨酸激酶 (BTK) 抑制剂。2-(Bromomethyl) acrylic acid 可通过亲核加成-消除反应与 BTK 的半胱氨酸 481 (Cys481) 残基形成共价键,从而抑制下游 B 细胞受体信号通路。2-(Bromomethyl) acrylic acid 可通过释放包括细胞外 ATP 和 HMGB1 在内的损伤相关分子模式,在表达 BTK 的 B 细胞淋巴瘤细胞中诱导免疫原性细胞死亡。2-(Bromomethyl) acrylic acid 对表达 BTK 的 B 细胞淋巴瘤细胞具有细胞毒性,而对 BTK 阴性细胞的毒性较低。2-(Bromomethyl) acrylic acid 可用于 B 细胞淋巴瘤的相关研究。

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2-(Bromomethyl)acrylic acid

2-(Bromomethyl)acrylic acid Chemical Structure

CAS No. : 72707-66-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

2-(Bromomethyl) acrylic acid is a Bruton's tyrosine kinase (BTK) inhibitor. 2-(Bromomethyl) acrylic acid forms a covalent bond with the cysteine 481 (Cys481) residue of BTK via a nucleophilic addition-elimination reaction, thereby inhibiting the downstream B-cell receptor signaling pathway. 2-(Bromomethyl) acrylic acid induces immunogenic cell death in BTK-expressing B-cell lymphoma cells by releasing damage-associated molecular patterns including extracellular ATP and HMGB1. 2-(Bromomethyl) acrylic acid exhibits cytotoxicity against BTK-expressing B-cell lymphoma cells, but shows low toxicity to BTK-negative cells. 2-(Bromomethyl) acrylic acid can be used in studies related to B-cell lymphoma[1].

体内研究
(In Vivo)

Ibt-DOX (2.5 mg/kg; i.v.; once every 2 days; 14 days) 可使雌性 SCID 小鼠的皮下 OCI-LY10 异种移植瘤体积降低 54%,且未观察到显著的体重下降或毒性[1]

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

Animal Model: SCID (female)[1]
Dosage: 2.5 mg/kg
Administration: i.v.; once every 2 days; 14 days
Result: Reduced average tumor size by 54% compared to the vehicle group.
Showed no significant body weight change or poisoning symptoms.
分子量

164.99

Formula

C4H5BrO2

CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
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The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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  • 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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2-(Bromomethyl)acrylic acid
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HY-W017180
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