Cytotoxicity Kinetics Compared
(To see more detail data of the hemiasterlins alone, see this.)
 
Drug Target
etoposide, doxorubicin, mitoxantrone DNA/topoisomerase II
vinblastine, hemiasterlin /A/C,
paclitaxel, dolastatin 10		 Tubulin

SUMMARIES
IC50s are the concentrations at which
growth is 50% of that measured for
untreated cultures (100% growth) and
were derived from plots of % growth
inhibition vs. concentration for each time
point indicated. (Details)
(To see more detail data of the hemiasterlins
alone, see this.) 		Potency @ ~1-2 days:
  1. dolastatin 10
  2. paclitaxel / hemiasterlin
  3. hemiasterlin A / hemiasterlin C
  4. vinblastine / paclitaxel
  5. mitoxantrone
  6. doxorubicin
  7. etoposide
 Sensitivity:
MCF7  >  PC3  cells.
Kinetics:
Hemiasterlin /A/C approach
their max IC50s ~ as quickly
as dolastatin 10 – sooner
than paclitaxel or vinblastine;
see ratio bar charts below.

* BARS: Not std error indicators. Range of values for each point (mean), which varies by experiment and/or variation in controls (100% growth).

source

Details: Cultures were seeded at 1000-2000 cells per microtiter plate well and incubated ~16-24h before drugs were introduced in equal volumes of media. Fresh media was exchanged at the indicated times, and incubation proceeded for the balance of ~72 h, followed by 10% cold TCA precipitation then staining with sulforhodamine B (for total protein). Following destaining, A530 (plate reader) was the measure of growth. Drug concentrations at which the A530 of the retained, solublized stain was 50% of no-drug control values – IC50s – were determined by eye from %inhibition vs. log[drug] plots.

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