Table 1 BI 894999 effect on cell proliferation (alamarBlue® assay) for hematological cell lines

From: The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML

Indication

Cell line

EC50 (nM)

Mutation/Karyotype/Subtype

Experiments (n)

AML

HL-60

2.7 ± 0.1

MYC amplification

2

AML

Kasumi-1

2.8 ± 0.4

AML1-ETO

2

AML

Kasumi-3

3.4 ± 1.5

EVI1 overexpression

3

AML

KG-1

6.2 ± 2.2

NRAS

2

AML

MOLM-13

12.8 ± 3.4

MLL-AF9; FLT3-ITD

3

AML

MOLM-13 GFP

14.3

MLL-AF9; FLT3-ITD

1

AML

MUTZ-3

12.8 ± 11.2

EVI1 rearrangement

3

AML

MV-4-11B

6.8 ± 4.0

MLL-AF4; FLT3-ITD

9

AML

MV-4-11B GFP

2.9 ± 0.9

MLL-AF4; FLT3-ITD

4

AML

NOMO-1

5.7 ± 4.1

MLL-AF9

2

AML

OCI-AML3

2.3 ± 0.5

NPM1 gene mutation (type A) and DNMT3A R882C mutation

2

AML

SKM-1

10.2 ± 1.5

EZH2-Y641C

2

AML

THP-1

6.3 ± 2.9

MLL-AF9

3

AML

THP-1 GFP

4.1 ± 2.0

MLL-AF9

2

CML

K562

>10,000

 

2

CML

MOLM-1

53.4 ± 34.8

EVI1 overexpression

3

T-ALL

CCRF-CEM

175 ± 58

 

2

T-ALL

J.RT3-T3.5

11 ± 4

 

2

T-ALL

MOLT-3

14.4 ± 6.5

 

2

T-ALL

MOLT-4

40.7 ± 28.7

 

2

MM

AMO-1

28 ± 15

Plasmacytoma

3

MM

L-363

13.7 ± 6.2

t(11;14)

2

MM

MM.1R

2.5 ± 2.1

t(14;16)

2

MM

MOLP-8

5.3 ± 2.8

t(11;14)

9

MM

MOLP-8 GFP

21.5 ± 10.8

t(11;14)

4

MM

NCI-H929

3.6 ± 2.0

t(4;14)

2

MM

OPM-2

8.9 ± 4.7

t(4;14)

2

MM

OPM-2 GFP

12

t(4;14)

1

MM

RPMI 8226

25 ± 9

t(14;16)

3

MM

U266 B1

14.3 ± 7.4

 

6

Lymphoma

HBL-1

7.1 ± 5.2

DLBCL, ABC type

2

Lymphoma

OCI-Ly18

5.6 ± 0.9

DLBCL, ABC type

2

Lymphoma

OCI-Ly3

8.2 ± 2.3

DLBCL, ABC type

2

Lymphoma

Pfeiffer

10.7 ± 2.7

DLBCL, ABC type

2

Lymphoma

RI-1

6.2 ± 1.9

DLBCL, ABC type

2

Lymphoma

SU-DHL2

10.7 ± 3.2

DLBCL, ABC type

2

Lymphoma

TMD8

9.7 ± 3.7

DLBCL, ABC type

13

Lymphoma

Toledo

6.0 ± 1.1

DLBCL, ABC type

3

Lymphoma

U-2932

4.3 ± 2.1

DLBCL, ABC type

3

Lymphoma

DB

11.6 ± 7.6

DLBCL, GCB type

2

Lymphoma

DOHH-2

6.2 ± 0.8

DLBCL, GCB type

2

Lymphoma

HT

11.6 ± 8.1

DLBCL, GCB type

2

Lymphoma

OCI-Ly7

14.2 ± 6.4

DLBCL, GCB type

2

Lymphoma

OCI-Ly19

13.2 ± 4.3

DLBCL, GCB type

4

Lymphoma

RC-K8

7.8 ± 0.9

DLBCL, GCB type

2

Lymphoma

RL

18.2 ± 10.0

DLBCL, GCB type

2

Lymphoma

SU-DHL4

13.3 ± 4.5

DLBCL, GCB type

3

Lymphoma

SU-DHL6

13.4 ± 1.2

DLBCL, GCB type

2

Lymphoma

MHH-PREB-1

24.4 ± 1.2

B cell lymphoma

2

Lymphoma

JEKO-1

7.9 ± 2.1

Mantle cell lymphoma

2

Lymphoma

DERL-2

10.6 ± 9.5

T cell lymphoma

2

Lymphoma

HuT78

7.1 ± 3.7

T cell lymphoma

3

Lymphoma

SR-786

77.3 ± 17.3

Anaplastic large-cell lymphoma

2

  1. EC50 (mean and S.D.)