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A new type of carbon dots (CD-Asp) with targeting function toward brain cancer glioma was synthesized via a straightforward pyrolysis route by using d-glucose and l-aspartic acid as starting materials. The as-prepared CD-Asp exhibits not only excellent biocompatibility and tunable full-color emission, but also significant capability of targeting C6 glioma cells without the aid of any extra targeting molecules. In vivo fluorescence images showed high-contrast biodistribution of CD-Asp 15 min after tail vein injection. A much stronger fluorescent signal was detected in the glioma site than that in normal brain, indicating their ability to freely penetrate the blood–brain barrier and precisely targeting glioma tissue. However, its counterparts, the CDs synthesized from d-glucose (CD-G), l-asparic acid (CD-A), or d-glucose and l-glutamic acid (CD-Glu) have no or low selectivity for glioma. Therefore, CD-Asp could act as a …