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.

H. pylori infection-induced apoptosis resistance in gastric epithelial cells triggered by Raptinal[1]. 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[1]. 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 IC 50 values between 0.7-3.4 μM, indicating activity across a wide variety of cell lines[2]. Cell Viability Assay[2]Cell Line: Human Lymphoma U-937, SKW 6.4, or Jurkat cell lines Concentration: 0.7-3.4 μM Incubation Time: 24 hours Result: The IC 50 values of Raptinal against U-937, SKW 6.4, or Jurkat cell lines were 1.1±0.1, 0.7±0.3, 2.7±0.9 μM, respectively. Western Blot Analysis[1]Cell Line: Human gastric cancer cell lines AGS, MKN28, MKN45 Concentration: 10?μM Incubation Time: 2 hours Result: Induced apoptosis by activating caspase-3 within 30?min at a concentration of 10?μM. Treatment with 10?μM of Raptinal for 2?h induced the cleavage of pro-caspase-3 into it’s active form in all three cell lines.

Raptinal is an unusually rapid inducer of caspase-dependent apoptosis in multiple cell lines and?in vivo?systems[1]. 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[2]. 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[2]. Animal Model: C57BL/6 and BALB/c female mice (6-8 weeks old) bearing the B16-F10 model or 4T1 models[2]Dosage: 20 mg/kg Administration: Administered intraperitoneally; once daily for 3 consecutive days for B16-F10 and 4 consecutive days for 4T1 models Result: Retard tumor volume and tumor mass by 60% relative to controls in the B16-F10 model. Similar efficacy was observed for the 4T1 murine breast cancer tumor model with 50% growth inhibition after treatment.

1176-09-6

C28H18O2

386.44

Raptinal

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years