Liu Yang, a 33-year-old fighter pilot, will join two other astronauts aboard the Shenzhou 9 spacecraft when it lifts off from a remote Gobi Desert launch site on Saturday evening.
They will attempt a manned docking for the first time with the Tiangong (Heavenly Palace) 1 module, launched last September and part of China's exploratory preparations for a space lab.
Rendezvous and docking exercises between the two vessels will be an important hurdle in China's efforts to acquire the technological and logistical skills needed to run a full space lab that can house astronauts for long stretches.
Beijing is still far from catching up with the established space superpowers: the United States and Russia. The Tiangong 1 is a trial module, not the building block of a space station.
But the docking mission will be the latest show of China's growing prowess in space, alongside its growing military and diplomatic presence, and comes while budget restraints and shifting priorities have held back U.S. manned space launches.
Speaking to the official Xinhua news agency, Liu said she "yearns to experience the wondrous, weightless environment of space, see the Earth and gaze upon the motherland".
"Thank you for the confidence put in my by the motherland and the people, for giving me this chance to represent China's millions of women by going into space," Liu later told reporters at the Jiuquan launch center.
Medical experts who helped select the crew of the Shenzhou 9, have said that female astronauts must meet the same criteria as men, and then some, according to the China Daily.
Female Chinese astronauts must be married and preferably be mothers, the newspaper said, citing concerns that radiation would "harm their fertility".
Liu, from the poor and populous central province of Henan, has been praised in state media for her nerves of steel after safely landing her fighter jet after a bird strike that left the cockpit glass covered with blood.
China's latest space mission has attracted even more than the usual national attention thanks to Liu's presence.
Her selection to the mission team rapidly became the top subject on the country's Twitter-like microblogging service Sina Weibo, with 33 million posts.
"Liu Yang, on the eve of becoming our first woman is space, is the pride of Henan," wrote one user.
But others wondered if the money poured into space ambitions would be better used on Earth, where China is still a developing country and grappling with more mundane issues like food safety and a growing rich-poor divide.
"What use does Shenzhou 9 have? Will it help the people to not starve?" another user wrote.