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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.