Table 1 IC50 values (in nM) for anti-proliferative activities of novel compounds on HGSOC mouse models BR-Luc and BR-5 compared to cisplatin.

From: Targeted therapy of pyrrolo[2,3-d]pyrimidine antifolates in a syngeneic mouse model of high grade serous ovarian cancer and the impact on the tumor microenvironment

Inhibitor

BR-Luc

BR-5

IGROV1

No addition

Folic acid (200 nM)

No addition

Folic acid (200 nM)

No addition

Folic acid (200 nM)

Cisplatin

290 ± 170

ND

160 ± 110

ND

857 ± 62

ND

AGF94

5.86 ± 3.67

249 ± 123

8.10 ± 4.90

346 ± 166

4.14 ± 0.94

195 ± 29

AG278

6.06 ± 3.12

588 ± 163

6.55 ± 3.24

547 ± 188

1.90 ± 0.15

426 ± 152

AG283

75.52 ± 33.28

639 ± 165

63 ± 14

598 ± 158

5.61 ± 1.20

242 ± 106

  1. In vitro proliferation assays were performed for BR-5 and BR-Luc mouse HGSOC tumor cells (both express RFC, FRα, and PCFT). Anti-proliferative studies were performed in folate-free RPMI1640 media with 10% dialyzed FBS and 25 nM leucovorin. To measure FR-mediated drug delivery, experiments were performed in the presence or absence of 200 nM folic acid. Results are presented as IC50 values, corresponding to the concentrations that inhibit growth by 50% relative to cells incubated without drug. The data are presented as mean values from at least 3 experiments (± standard errors). The pyrrolo[2,3-d]pyrimidine antifolates were previously described21,22.
  2. ND not done.
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