Raptinal

Raptinal is a cytotoxic agent on cancer cells, rapidly activating the intrinsic apoptotic pathway and simultaneously shuting down mitochondrial function, bypassing BAX, BAK, and BOK for mitochondrial outer membrane permeabilization and intrinsic apoptosis 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.

Product information

CAS Number: 1176-09-6

Molecular Weight: 386.44

Formula: C28H18O2

Chemical Name: 9-(9-Formylfluoren-9-yl)fluorene-9-carbaldehyde

Smiles: O=CC1(C2=CC=CC=C2C2=CC=CC=C12)C1(C=O)C2=CC=CC=C2C2=CC=CC=C12

InChiKey: GLANOOJJBKXTMI-UHFFFAOYSA-N

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

H. pylori infection-induced apoptosis resistance in gastric epithelial cells triggered by Raptinal. 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. 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.

In Vivo:

Raptinal is an unusually rapid inducer of caspase-dependent apoptosis in multiple cell lines and in vivo systems. 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. 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.

References:

1. Rahul Palchaudhuri,et al. A Small Molecule that Induces Intrinsic Pathway Apoptosis with Unparalleled Speed. Cell Rep. 2015 Dec 1;13(9):2027-36.
2. Yanheng Chen, et al. H. pylori infection confers resistance to apoptosis via Brd4-dependent BIRC3 eRNA synthesis. Cell Death Dis. 2020 Aug 21;11(8):667.

Products are for research use only. Not for human use.