S2. Best tumor response.

Response	n (%)
	Escalation cohort (N=15)						Expansion cohort (N=20)
	50 mg/d (N=3)*	100 mg/d (N=2)	150 mg/d (N=2)	200 mg/d (N=3)	250 mg/d (N=5)		100 mg/d (N=11)	200 mg/d (N=9)
*, Tumor response analysis was based on the per-protocol set (PPS). CR, complete response; PR, partial response; SD, stable disease; PD, progressive disease; ORR, objective response rate; DCR, disease control rate.
CR	0 (0)	0 (0)	0 (0)	0 (0)	0 (0)		0 (0)	0 (0)
PR	0 (0)	0 (0)	0 (0)	1 (33.3)	0 (0)		1 (9.1)	2 (22.2)
SD	3 (100)	0 (0)	1 (50.0)	1 (33.3)	3 (60.0)		6 (54.5)	6 (66.7)
PD	0 (0)	2 (100)	1 (50.0)	1 (33.3)	2 (40.0)		4 (36.4)	1 (11.1)
ORR	0 (0)	0 (0)	0 (0)	1 (33.3)	0 (0)		1 (9.1)	2 (22.2)
DCR	3 (100)	0 (0)	1 (50.0)	2 (66.7)	3 (60.0)		7 (63.6)	8 (88.9)