| Chemical Properties | Back Directory | [Melting point ]
219 °C | [Boiling point ]
531.3±50.0 °C(Predicted) | [density ]
1.378±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 33.33 mg/mL (86.25 mM; Need ultrasonic) | [form ]
powder to crystal | [color ]
White to Almost white |
| Hazard Information | Back Directory | [Uses]
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 th at 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). | [Biological Activity]
Raptinal is a cell-permeable bifluorene-dicarbaldehyde compound th at acts as a rapid activator of mitochondrial pathway-mediated intrinsic apoptosis. | [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.?
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| [IC 50]
Caspase 3 | [storage]
Store at -20°C |
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| Company Name: |
TCI Chemicals
|
| Tel: |
021-67121386, 800-988-0390 |
| Website: |
www.tcichemicals.com |
| Company Name: |
Wuhan Topule
|
| Tel: |
+86-02787215551 +86-19945035818 |
| Website: |
http://www.topule.com/ |
|