1. Apoptosis
  2. Caspase
  3. Raptinal

Raptinal 

Cat. No.: HY-121320
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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.

For research use only. We do not sell to patients.

Raptinal Chemical Structure

Raptinal Chemical Structure

CAS No. : 1176-09-6

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Description

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[1][2].

IC50 & Target[1]

Caspase 3

 

In Vitro

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 IC50 values between 0.7-3.4 μM, indicating activity across a wide variety of cell lines[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 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. 
In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. 
Molecular Weight

386.44

Formula

C₂₈H₁₈O₂

CAS No.
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Raptinal
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