Raptinal 直接激活 caspase-3，可启动 caspase 依赖性的细胞凋亡内源性途径。Raptinal 能够通过直接激活效应 caspase-3来快速诱导癌细胞死亡，绕过启动子 caspase-8 和 caspase-9的激活。 应用： Raptinal 在 30 分钟内（10 μM）完全释放细胞色素 c，并在一小时内激活 caspase-3。尽管在癌症和非癌细胞培养中均具有一般的细胞毒性（24 小时内细胞死亡诱导 EC50 = 0.6-3.4 μM），但小鼠单次 60 mg/kg 静脉注射 7 天后未观察到血液学毒性。研究表明，每日腹腔注射剂量（20 mg/kg）可有效抑制小鼠 B16-F10 黑色素瘤和 4T1 乳腺癌在体内的扩大（分别在 6 天内分别降低约 60％ 和 50％）。 Raptinal, a agent that directly activates caspase-3, initiates intrinsic pathway caspase-dependent apoptosis. Raptinal is able to rapidly induce cancer cell death by directly activating the effector caspase-3, bypassing the activation of initiator caspase-8 and caspase-9. Application： Raptinal showed complete cytochrome c release within 30 minutes and caspase-3 activation within one hour of exposure (10 μM). Despite its general cytotoxicity in both cancer and non-cancer cell cultures (Cell death induction EC50 = 0.6-3.4 μM in 24 hr), no hematologic toxicity was observed 7 days following single 60 mg/kg i.v. dosing in mice. Studies show that daily i.p. injection (20 mg/kg) is efficacious in suppressing murine B16-F10 melanoma and 4T1 breast cancer expansion in vivo (by ~60% and 50% in 6 days, respectively).
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Raptinal
CAS number：1176-09-6 molecular formula：C28H18O2
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Specs
| Chinese alias | [9,9'-二-9H-芴]-9,9'-二甲醛 | 拉普提纳尔 | 9H,9′H-9,9′-联芴-9,9′-二甲醛 | ||
| English alias | [9,9'-Bi-9H-fluorene]-9,9'-dicarboxaldehyde | ||
| CAS number | 1176-09-6 | molecular formula | C28H18O2 |
| molecular weight | 386.45 g/mol | Exact mass | ≥96%(HPLC) |
| PSA | 34.100 Ų | logp | 4.900 |
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