435300

LFM-A13

A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton′s Tyrosine Kinase (BTK; IC₅₀ = 17.2 µM for human BTK in vitro and IC₅₀ = 2.5 µM for recombinant BTK).

• 동의어(들): LFM-A13, α-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide, BTK Inhibitor I, Bruton′s Tyrosine Kinase Inhibitor I
• 실험식(Hill 표기법): C₁₁H₈Br₂N₂O₂
• CAS Number: 62004-35-7
• Molecular Weight: 360.00
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥97% (HPLC)
• 형태: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: light brown
• solubility: DMSO: 200 mg/mL
• 배송 상태: ambient
• 저장 온도: 2-8°C
• InChI: 1S/C11H8Br2N2O2/c1-6(16)8(5-14)11(17)15-10-4-7(12)2-3-9(10)13/h2-4,16H,1H3,(H,15,17)
• InChI key: UVSVTDVJQAJIFG-UHFFFAOYSA-N

설명

일반 설명

A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton’s Tyrosine Kinase (BTK; IC₅₀ = 17.2 µM for human BTK in vitro and IC₅₀ = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC₅₀ = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.

A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton′s tyrosine kinase (BTK; IC₅₀ = 17.2 µM for human BTK in vitro and IC₅₀ = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC₅₀ = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
Human Bruton′s Tyrosine Kinase (BTK)

Product competes with ATP.

Reversible: yes

Target IC₅₀: 17.2 µM for human BTK in vitro and 2.5 µM for recombinant BTK

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

기타 정보

Uckun, F.M., et al. 2006. Bioorg. Med. Chem. In press.
Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable