Gemcitabine 95058-81-4

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Molecular Weight:

263.2 Gemcitabine is a very potent and specific deoxycytidine analogue, used as chemotherapy.

Biological Activity

Gemcitabine results in 50% inhibition of growth in the CCRF-CEM human
leukemia cell culture assay with IC50 of 1 ng/ml. Gemcitabine combined
with deoxycytidine provides about a 1000-fold decrease in biological
activity. Gemcitabine combined with C225 results in
additive cytotoxic effects that increased with increasing gemcitabine
concentrations in human pancreatic carcinoma L3.6pl cells. Gemcitabine combined with Cisplatin results in synergistic effect in wild-type A2780 and cisplatin-resistant ADDP cells.


Gemcitabine combined with C225 results in growth inhibition, tumor
regression, and abrogation of metastasis in L3.6pl tumors established in
the pancreas of nude mice. Gemcitabine treatment alone reduces median
tumor volume from 538 to 152 mm3.


Gemcitabine reduces the production of vascular endothelial growth factor and interleukin 8 in gemcitabine-treated tumors. Gemcitabine is able to dramatically and specifically reduces the number
of myeloid suppressor cells found in the spleens of animals bearing
large tumors with no significant reductions in CD4(+) T cells, CD8(+) T
cells, NK cells, macrophages, or B cells.


Gemcitabine
combined with curcumin shows significant reductions in volume (P = 0.008
versus control; P = 0.036 versus gemcitabine alone), Ki-67
proliferation index (P = 0.030 versus control), NF-kappaB activation,
and expression of NF-kappaB-regulated gene products (cyclin D1, c-myc,
Bcl-2, Bcl-xL, cellular inhibitor of Apoptosis protein-1,
cyclooxygenase-2, matrix metalloproteinase, and vascular endothelial
growth factor) compared with tumors from control mice treated with olive
oil only. Gemcitabine combined with Curcumin is also highly effective
in suppressing Angiogenesis as indicated by a decrease in CD31(+)
microvessel density.

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