A field of molecular therapeutics has significantly advanced the treatment of many complex conditions, including cancer therapeutics. However many molecular formulations still lack the diagnostic power of tomography-guided approaches, and are restricted by dose-limiting toxicity. Multiple gene therapeutics, which have shown to be effective on a cellular level, require to be delivered in-vivo to protect the payload from degradation in blood. This technical gap outlines a clear need for multifunctional delivery/imaging agents. Nanomaterials provide these capabilities, safely delivering therapeutics concomitantly imaging their delivery pathways. Recently graphene derivatives (mainly, graphene oxide) became a focus of intense scientific inquiry including their applications in the biomedical field. Graphene Oxide (GO) is an attractive candidate for bioimaging due to its intrinsic fluorescence in the red/near-infrared spectral region with reduced biological autofluorescence background. This provides the capability of fluorescence imaging without the need for additional fluorophores. Additionally GO has a large platform for functionalization with drug molecules, is water soluble and exhibits pH-mediated response in its fluorescence emission. Nanoscale graphene oxide derivatives (NGO) produced via biocompatible bottom-up synthetic route have properties similar to GO, however, possessing a smaller size for more efficient cellular internalization. We explore these properties to develop a family of graphene-based imaging/sensing/delivery platforms for molecular therapeutics. GO or NGO utilized in our work show little to no cytotoxicity quantified via MTT assay up to the maximum imaging concentrations of 15 ug/mL. We use spectrally-resolved fluorescence imaging for in-vitro detection in the spectral ranges specific to GO or NGO emission. Both GO and NGO exhibit efficient cellular internalization assessed via their emission within HeLa cells, with significantly higher accumulation observed for NGO, suggesting a high potential for drug delivery applications and image-guided therapy. A pH dependence of both GO and NGO emission provides a sensing mechanism for the acidic environments of cancer cells; as many cancer cell types excrete lactic acid, their environments are more acidic than those of healthy cells. The difference between fluorescence in healthy (HEK-293)/cancer (HeLa, MCF-7) cell environments is quantified for graphene derivatives in this work via assessing the shifts in emission and/or variations in emission intensities at different wavelengths. As a result we propose a family of graphene derivatives, including GO and NGO functionalities, as efficient multifunctional candidates for in-vitro delivery of active agents, fluorescence imaging and pH-sensing of cancerous environments.