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Table 1 Determination of LC50 and IC50 values for BGT226, BKM120 and RAD001 in breast cancer cells

From: Preclinical modeling of combined phosphatidylinositol-3-kinase inhibition with endocrine therapy for estrogen receptor-positive breast cancer

Cell line ER status Genotype BGT226 (nmol/l) BKM120 (nmol/l) RAD001 (nmol/l)
    LC50 IC50 LC50 IC50 LC50 IC50
MCF7 Positive PIK3CA E545K 7.5 3.5 3,981 248 >625 >625
T47D Positive PIK3CA H1047R 10 2.7 316 128 >625 1.5
HCC712 Positive PIK3CB amp 549 >625 >10,000 347 >625 >625
MCF7 LTED Positive PIK3CA E545K 398 1.18 2,691 70.7 >625 <1
MCF7 LTED-R Positive PIK3CA E545K 617 5.1 >10,000 4,926 >625 >625
T47D LTED Negativea PIK3CA H1047R 19 2.3 630 243 >625 <1
BT-483 Positive PIK3CA E542K 2.5 7.05 >10,000 >10,000 >625 <1
MDA-MB-415 Positive PTEN mut 28.1 <1 1,584 1,294 >625 >625
CAMA-1 Positive PTEN mut 275 46.2 >10,000 >10,000 >625 <1
ZR75-1 Positive PTEN mut 1.3 <1 363 207 >625 <1
HCC1428 Positive PIK3CA/PTEN wt 501 >625 1,258 1,138 3.1 <1
MDA-MB-175 Positive PIK3CA/PTEN wt >625 <1 5,011 >10,000 >625 <1
MDA-MB-231 Negative K-Ras, B-Raf mut >625 <1 >10,000 1,237 >625 >625
  1. Cell lines growing under estrogen-deprived conditions in CSS medium were incubated with solvent control or increasing concentrations of the indicated compounds and cell viability was assessed at 0 hours (time of drug addition) and at 96 hours after treatment. PIK3CA, PIK3CB and PTEN mutation information has been published previously [5, 22] or was obtained from the Sanger website [31]. ER, estrogen receptor; IC50, half maximal inhibitory concentration; LC50, 50% lethal concentration; mut, mutant; wt, wild-type. aER was not detectable by western blot.