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)

Cat. No.: HY-W017180
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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.

For research use only. We do not sell to patients.

2-(Bromomethyl)acrylic acid

2-(Bromomethyl)acrylic acid Chemical Structure

CAS No. : 72707-66-5

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Based on 1 publication(s) in Google Scholar

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Description

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].

In Vivo

Ibt-DOX (2.5 mg/kg; i.v.; once every 2 days; 14 days) reduces subcutaneous OCI-LY10 xenograft tumor volume by 54% in female SCID mice, with no significant weight loss or toxicity observed[1].

MedChemExpress (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.
Molecular Weight

164.99

Formula

C4H5BrO2

CAS No.
Appearance

Solid

SMILES

C=C(C(O)=O)CBr

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
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    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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