The Food and Drug Administration has approved the product, developed by Blaze Bioscience, for study in human trials in the US.
During the phase one trial, the tumour paint will be used on an estimated 21 people with a glioma, or tumour in the brain or spine, 'ABC News' reported.
The 'paint' will light up the tumour with special florescent molecules, allowing surgeons to remove cancerous tissue more effectively and safely.
The paint is developed by utilising a protein derived from the paralysing venom of an Israeli deathstalker scorpion.
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"It's really hard to get molecules into the brain due to the blood-brain barrier," said Dr Jim Olsen, a brain cancer specialist at Seattle Children's Hospital and a professor at the Fred Hutchinson Cancer Research Centre in Seattle.
"Most drugs that are made by the drug companies can't penetrate that barrier. The scorpion has found a way to get these proteins in the brain," said Olson, who developed the product.
Olson said that in earlier canine trials, the paint was able to show small amounts of cancer cells that would be nearly impossible to identify with the human eye.