1176-09-6
1176-09-6 structure
- Name: Raptinal
- Chemical Name: 9,9'-diformyl-9,9'-bifluorenyl
- CAS Number: 1176-09-6
- Molecular Formula: C28H18O2
- Molecular Weight: 386.44
- Catalog: Signaling Pathways Apoptosis Caspase
- Create Date: 2018-05-25 01:53:27
- Modify Date: 2024-01-09 16:46:52
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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[1][2].
| Name | 9,9'-diformyl-9,9'-bifluorenyl |
|---|---|
| Synonyms |
[9,9']bifluorenyl-9,9'-dicarbaldehyde
[9,9']Bifluorenyl-9,9'-dicarbaldehyd α.α'-Bis-diphenylen-succindialdehyd 9.9'-Diformyl-difluorenyl-(9.9') 9,9'-Biformyl-9,9'-bifluorenyl 9.9'-Diformyl-9.9'-bifluorenyl |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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]. 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]. 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. |
| References |
| Melting Point | 219 °C |
|---|---|
| Molecular Formula | C28H18O2 |
| Molecular Weight | 386.44 |
| Exact Mass | 386.13100 |
| PSA | 34.14000 |
| LogP | 5.31760 |