| MELK |
OTS167 |
Multiple |
DU4475 (2.3), T47D (4.3), 22Rv1 (6.0), A549 (6.7) |
In A549 xenograft, 10 mg kg–1 IV injection once a day for 14 days → 108% TGI on day 15; 10 mg kg–1 PO administration once a day for 14 days → 124% TGI on day 15 |
22
|
| AML |
MV4-11 (7.9), THP-1 (15.6), KG1 (16.9), KOCL-48 (16.9), MOLM13 (17.5), KG1a (26.4), K562 (33.0), ML-2 (33.8), U937 (69.8) |
|
24
|
| Gastric cancer |
BGC823 (25), SGC7901 (25) |
In two MELK-positive PDX models, 15 mg kg–1 IV injection once every two days for 14 days → 106% and 112% TGI on day 15 |
28
|
| SCLC |
H69 (0.8), H82 (1.7), H524 (1.9), DMS114 (2.1), SBC5 (2.8), SBC3 (4.3), H69AR (4.4), H2171 (4.7), H446 (6.2), H146 (7.9), DMS273 (8.4) |
|
25
|
| Kidney cancer |
Caki-1 (12.4), 769-P (20.1), 786-O (23.9), VMRC-RCW (25.5), Caki-2 (38.7) |
|
26
|
| TOPK |
OTS514 |
Multiple |
LU-99 (1.5), Daudi (3.7), MKN1 (4.6), HCT-116 (4.8), MIAPaca-2 (5.2), UM-UC-3 (5.7), MKN45 (6.1), DU4475 (6.4), A549 (6.5), 22Rv1 (8.0), T47D (8.4), HepG2 (8.5), MDA-MB-231 (14) |
In A549 xenograft, 5 mg kg–1 IV injection once a day for 14 days → 65% TGI on day 15; in LU-99 xenograft, 5 mg kg–1 IV injection once a day for 14 days → 104% TGI on day 15, but caused reduction of WBCs |
34
|
| AML |
KOCL-48 (7.1), MOLM13 (9.0), MV4-11 (10.7), ML-2 (17.9), U937 (19.2), THP-1 (23.5), KG1a (26.2), K562 (36.8), KG1 (48.7) |
In MV4-11 engrafted xenograft, 7.5 mg kg–1 IV injection once a day for 21 days → significantly elongated overall survival of mice (P < 0.001) |
29
|
| Kidney cancer |
VMRC-RCW (19.9), Caki-2 (20.1), 769-P (20.7), Caki-1 (27.8), 786-O (44.1) |
|
26
|
| Ovarian cancer |
CaOV3 (5.1), PA-1 (5.0), ES-2 (5.6), SKOV3 (6.3), OV90 (8.8), SW626 (9.4), OVCAR3 (12), A2780 (10), OVSAHO (13), RMG-I (15), OVTOKO (46) |
In ES-2 abdominal dissemination xenograft, 25 mg kg–1 PO administration once a day for 14 days → significantly elongated overall survival of mice (P < 0.001) |
30
|
| OTS964 |
Multiple |
LU-99 (7.6), HepG2 (19), Daudi (25), MIAPaca-2 (30), A549 (31), UM-UC-3 (32), HCT-116 (33), MKN1 (38), MKN45 (39), 22Rv1 (50), DU4475 (53), T47D (72), MDA-MB-231 (73) |
In LU-99 xenograft, 40 mg kg–1 IV injection of liposomal OTS964 five times for 14 days → 110% TGI on day 15, and complete regression of tumors in 5 of 6 mice by day 29; 100 mg kg–1 PO administration once a day for 14 days → 113% TGI on day 15, and complete regression of tumors in all 6 mice by day 29 |
34
|
| TTK |
TTK-27f |
Multiple |
MKN45 (3.3), LU-99 (4.7), GSS (5.3), A549 (6.0), LU-116 (6.1), HCT15 (6.3), MIAPaca-2 (8.1), HL60 (9.1), HCT116 (9.4), PC-14 (9.8), NCI-H460 (10), HT29 (16), LC2/ad (17) |
In NCI-H460 xenograft, 10 mg kg–1 PO administration once a day for 14 days → 81% TGI on day 15, but caused body weight loss and 3 of 6 mice died on day 11 |
46
|
