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。

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.

Solid

Caspase 3

H. pylori  infection-induced apoptosis resistance in gastric epithelial cells triggered by Raptinal. 
Treatment with 10?μM of Raptinal for 2?h induces the cleavage of pro-caspase-3 into it’s active form in human gastric cancer cell lines AGS, MKN28, MKN45.
Raptinal initiates intrinsic pathway caspase-dependent apoptosis within minutes in multiple cell lines. Raptinal induces death against various cancer and non-cancerous cell lines with 24 hour IC50 values between 0.7-3.4 μM, indicating activity across a wide variety of cell lines. has not independently confirmed the accuracy of these methods. They are for reference only.

Raptinal is an unusually rapid inducer of caspase-dependent apoptosis in multiple cell lines and in vivo systems.
Raptinal (20 mg/kg; administered intraperitoneally; once daily for 3 consecutive days for B16-F10 and 4 consecutive days for 4T1 models) exerts anticancer activity in vivo.
C57BL/6 mice are administered intravenous Raptinal across a range of dosages as a one-time injection. When administered intravenously at a dosage of 37.5 mg/kg, the peak plasma concentration and elimination half-life of Raptinal are 54.4±0.9 μg/mL and 92.1±5.8 minutes, respectively. Single-dose intravenous Raptinal is well tolerated across a wide dose range (15-60 mg/kg) and does not cause hematologic toxicity as assessed 7 days post-administration. has not independently confirmed the accuracy of these methods.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Yanheng Chen, et al. H. pylori infection confers resistance to apoptosis via Brd4-dependent BIRC3 eRNA synthesis. Cell Death Dis. 2020 Aug 21;11(8):667.
[2]. Rahul Palchaudhuri,et al. A Small Molecule that Induces Intrinsic Pathway Apoptosis with Unparalleled Speed. Cell Rep. 2015 Dec 1;13(9):2027-36.

In Vitro: DMSO : 20 mg/mL (51.75 mM; ultrasonic and warming and heat to 60°C)配制储备液