Table 1 LSN3213128 activity in tissue culture.

From: Characterization of a novel AICARFT inhibitor which potently elevates ZMP and has anti-tumor activity in murine models

Cell line

ZMP EC50 (nM) Low folate

ZMP EC50 (nM) Regular folate

Alamar Blue GI50 (nM) Low folate

Alamar Blue GI50 (nM) Regular folate

HCT 116 (colon)

2.7 ± 3.3

369 ± 44

2.2 ± 2.1

2811 ± 1220

SW620 (colon)

4.3 ± 0.9

600

8.8 ± 1.6

3910 ± 3239

SNU-16 (gastric)

2

2500

1.2 ± 1.2

1590 ± 1273

A549 (lung)

10

3100

6

NCI-H1155 (lung)

2.3

380

4.9

729 ± 215

NCI-H1299

4.1

4.8

1590

NCI-H1437 (lung)

4.6

620 ± 354

0.73

1883 ± 894

NCI-H1993 (lung)

7.1

3.0 ± 2.7

2676 ± 2537

NCI-H460 (lung)

8

428 ± 102

16.4 ± 5.1

3470 ± 2092

MDA-MB-231 (mammary)

7.6

89

0.49

85 ± 42

A101D (melenoma)

2.3

2.9

3290

MIA PaCa-2 (pancreas)

4.2

1700

1.6 ± 1.0

4870 ± 4200