Canfosfamide-TLK-286-DataSheet-生命科学试剂-MCE.pdf

Hotline: 400-820-3792 Inhibitors • Screening Libraries • Proteins www.MedChemE Canfosfamide Cat. No.: HY-16124 CAS No.: 158382-37-7 Synonyms: TLK-286; TER286 分⼦式: C₂₆H₄₀Cl₄N₅O₁₀PS 分⼦量: 787.47 作⽤靶点: DNA-PK; Apoptosis 作⽤通路: Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Apoptosis 储存⽅式: Please store the product under the recommended conditions in the Certificate of Analysis. BIOLOGICAL ACTIVITY ⽣物活性 Canfosfamide (TLK-286) 是⼀种⾕胱⽢肽类似物前体药物，由⾕胱⽢肽 S-转移酶 P1-1 激活，诱导细胞凋亡 ( apoptosis)。Canfosfamide还抑制 DNA 依赖性蛋⽩激酶 (DNA-PK) 的催化激酶活性。Canfosfamide 在活化后 产⽣⼀种抗癌烷基化剂和⾕胱⽢肽衍⽣物。Canfosfamide 可⽤于恶性肿瘤的研究。 IC50 Target IC50: ~1 µM (DNA-PK) [3] 体外研究 Canfosfamide (TLK-28) inhibit the catalytic kinase activity of purified DNA-dependent protein kinase (DNA- PK) with an IC50 value of ~1 µM, but causes minimal direct damage to DNA [2]. Canfosfamide (TER286) inhibits MCF-7, NIH-3T3 and M7609 in a dose-dependent manner [3]. Cell Proliferation Assay [3] Cell Line: MCF-7, NIH-3T3 and M7609 Concentration: 0-100 μM Incubation Time: Co-incubated for 2 h then removed and incubated for 5 days in MCF-7; co-incubated for 10 days in NIH-3T3; co-incubated for 48 h in M7609 Result: Inhibited thes