Raptinal

Product NameRaptinal
CAS1176-09-6
MFC28H18O2
MW386.44
EINECS
MOL File1176-09-6.mol

Chemical Properties

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
InChI	1S/C28H18O2/c29-17-27(23-13-5-1-9-19(23)20-10-2-6-14-24(20)27)28(18-30)25-15-7-3-11-21(25)22-12-4-8-16-26(22)28/h1-18H
InChIKey	GLANOOJJBKXTMI-UHFFFAOYSA-N
SMILES	O=CC(C1=C2C=CC=C1)(C3(C=O)C4=C(C5=C3C=CC=C5)C=CC=C4)C6=C2C=CC=C6

Safety Information

WGK Germany	WGK 2
HS Code	2912.29.6090
Storage Class	11 - Combustible Solids
Hazard Classifications	Eye Irrit. 2 Skin Irrit. 2 STOT SE 3

Usage And Synthesis

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.

IC 50

Caspase 3

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