Table 1 Effect of MRTX849 on the reversal of MDR mediated by ABCB1

Doxorubicin

0.029 ± 0.063

(1.00)

2.091 ± 0.046

(1.00)

 + MRTX849 (0.25 μM)

0.028 ± 0.091

(1.06)

1.503 ± 0.079*

(1.39)

 + MRTX849 (0.5 μM)

0.026 ± 0.076

(1.13)

0.929 ± 0.047**

(2.25)

 + MRTX849 (1 μM)

0.026 ± 0.020

(1.14)

0.331 ± 0.092**

(6.32)

 + Verapamil (10 μM)

0.027 ± 0.068

(1.11)

0.107 ± 0.089**

(19.46)

Paclitaxel

0.002 ± 0.036

(1.00)

0.580 ± 0.056

(1.00)

 + MRTX849 (0.25 μM)

0.002 ± 0.075

(1.00)

0.241 ± 0.080**

(2.41)

 + MRTX849 (0.5 μM)

0.002 ± 0.073

(1.06)

0.165 ± 0.064**

(3.53)

 + MRTX849 (1 μM)

0.002 ± 0.057

(0.96)

0.033 ± 0.038**

(17.81)

 + Verapamil (10 μM)

0.003 ± 0.080

(0.93)

0.027 ± 0.069**

(21.51)

Cisplatin

0.611 ± 0.024

(1.00)

2.579 ± 0.053

(1.00)

 + MRTX849 (1 μM)

0.608 ± 0.035

(1.01)

2.575 ± 0.056

(1.00)

Doxorubicin

0.380 ± 0.020

(1.00)

11.667 ± 0.405

(1.00)

 + MRTX849 (0.25 μM)

0.387 ± 0.062

(0.98)

5.812 ± 0.023**

(2.01)

 + MRTX849 (0.5 μM)

0.401 ± 0.048

(0.95)

2.386 ± 0.042**

(4.90)

 + MRTX849 (1 μM)

0.391 ± 0.093

(0.97)

1.596 ± 0.081**

(7.31)

 + Verapamil (10 μM)

0.376 ± 0.109

(1.01)

0.798 ± 0.012**

(14.61)

Paclitaxel

0.036 ± 0.010

(1.00)

1.070 ± 0.063

(1.00)

 + MRTX849 (0.25 μM)

0.035 ± 0.032

(0.97)

0.629 ± 0.060*

(1.70)

 + MRTX849 (0.5 μM)

0.033 ± 0.038

(0.96)

0.222 ± 0.059**

(4.83)

 + MRTX849 (1 μM)

0.028 ± 0.083

(1.58)

0.068 ± 0.191**

(15.85)

 + Verapamil (10 μM)

0.032 ± 0.072

(1.26)

0.052 ± 0.070**

(20.69)

Cisplatin

5.242 ± 0.075

(1.00)

6.630 ± 0.046

(1.00)

 + MRTX849 (1 μM)

5.172 ± 0.120

(1.01)

6.455 ± 0.154

(1.03)

Mitoxantrone

0.173 ± 0.038

(1.00)

6.497 ± 0.107

(1.00)

 + MRTX849 (0. 25 μM)

0.178 ± 0.065

(0.98)

6.527 ± 0.029

(0.99)

 + MRTX849 (0. 5 μM)

0.161 ± 0.096

(1.08)

6.558 ± 0.030

(0.99)

 + MRTX849 (1 μM)

0.191 ± 0.133

(0.92)

6.578 ± 0.061

(0.99)

 + FTC (2.5 μM)

0.142 ± 0.053

(1.21)

0.533 ± 0.040**

(12.19)

Topotecan

0.250 ± 1.082

(1.00)

8.950 ± 0.288

(1.00)

 + MRTX849 (0.25 μM)

0.274 ± 0.085

(0.92)

9.250 ± 0.097

(0.98)

 + MRTX849 (0.5 μM)

0.241 ± 0.073

(1.02)

9.206 ± 0.098

(0.98)

 + MRTX849 (1 μM)

0.281 ± 0.043

(0.89)

9.104 ± 0.079

(0.99)

 + FTC (2.5 μM)

0.251 ± 0.079

(0.98)

0.753 ± 0.074**

(11.93)

Cisplatin

10.152 ± 0.261

(1.00)

8.864 ± 0.116

(1.00)

 + MRTX849 (1 μM)

9.931 ± 0.221

(1.02)

8.501 ± 0.170

(1.02)

Doxorubicin

0.061 ± 0.004

(1.00)

1.218 ± 0.081

(1.00)

 + MRTX849 (0.25 μM)

0.059 ± 0.067

(1.03)

0.474 ± 0.074**

(2.57)

 + MRTX849 (0.5 μM)

0.059 ± 0.060

(1.02)

0.315 ± 0.061**

(3.87)

 + MRTX849 (1 μM)

0.061 ± 0.082

(1.00)

0.116 ± 0.067**

(10.47)

 + Verapamil (10 μM)

0.063 ± 0.055

(0.96)

0.075 ± 0.065**

(16.18)

Paclitaxel

0.029 ± 0.001

(1.00)

2.543 ± 0.086

(1.00)

 + MRTX849 (0.25 μM)

0.028 ± 0.071

(1.05)

1.643 ± 0.030*

(1.70)

 + MRTX849 (0.5 μM)

0.028 ± 0.099

(1.02)

0.670 ± 0.052**

(3.79)

 + MRTX849 (1 μM)

0.025 ± 0.049

(1.17)

0.030 ± 0.096**

(8.36)

 + Verapamil (10 μM)

0.026 ± 0.034

(1.09)

0.023 ± 0.182**

(11.19)

Cisplatin

1.840 ± 0.062

(1.00)

2.247 ± 0.109

(1.00)

 + MRTX849 (1 μM)

1.795 ± 0.010

(1.03)

2.148 ± 0.075

(1.05)