Table 1.
Drug | Selumetinib | Buparlisib | ||||
---|---|---|---|---|---|---|
Cell Line | SUM149 | MDA-MB-231Br | Combined | SUM149 | MDA-MB-231Br | Combined |
Dose (IC 25) | 200 nM | 5.04 µM | N/A | 810 nM | 850 nM | N/A |
Gene “Hits” |
BRAF, RAF1 (CRAF), MAP4K3, MAP2K1 (MEK1), MAP2K5, MAPK10, MAPK11
PIK3C2A, PIK3C3, PIK3CB, PIK3R4 PDGFRB CDK2, CDK3, CDK5, CDK6, AURKB, BUB1B EPHA1, EPHA3, EPHA4, EPHA6, EPHB1, EPHB3, EPHB4, EFNB3 INSR, FLT1 (VEGFR1), FGFR4, ERBB4, TGFBR2 |
BRAF, RAF1 (CRAF), MAP4K1, MAP4K3, MAP3K5, MAP3K7,
MAP3K12, MAP2K2 (MEK2), MAP2K7, MAPK1 (ERK2), MAPK4 (ERK4), MAPK7, MAPK10, RPS6KA2 (RSK3), RPS6KA4 (MSK2), RPS6KA5 (MSK1) PIK3C2B, AKT2, RPS6KB1 (S6K1) PDGFRB CDK2, CDK3, CDK4, CDK5, CDK5R1, CDK7, CDK9, CDK11, CHEK2 EPHA1, EPHA3, EPHA4, EPHA10, EPHB1, EPHB3, EPHB4 INSR, EGFR, FLT1 (VEGFR3), TGFBR2 |
BRAF, RAF1 (CRAF), MAP4K1, MAP4K3, MAP3K1, MAP3K3, MAP3K5, MAP3K6, MAP3K7, MAP3K10, MAP3K12,
MAP2K1 (MEK1), MAP2K2 (MEK2), MAP2K4, MAP2K5, MAP2K6, MAP2K7, MAPK1 (ERK2), MAPK10, MAPK11, RPS6KA1 (RSK1), RPS6KA5 (MSK1), DUSP21 PIK3CB, PIK3C2B, PIK3C3, PIK3CD, PIK3R4 PDGFRA, PDGFRB CDK2, CDK3, CDK5, CDK5R1, CDK6, CDK9, CDK11, AURKB, PLK3, DDR1, CHEK2 EPHA1, EPHA3, EPHA4, EPHA6, EPHB1, EPHB3, EPHB4 INSR, INSRR, FLT1 (VEGFR1), FGFR4, TGFBR2 |
MAP2K1 (MEK1) AURKA, BUB1 |
BRAF, RAF1 (CRAF), TAO1 (TAOK1),
MAP4K3, MAP3K5, MAP3K13, MAP3K14, MAP2K7, MAPK6 (ERK3), RPS6KA1 (RSK1), RPS6KA3 (RSK2) AKT2, RPS6KB1 (S6K1) AURKC, BUB1, BUB1B, PLK3, DDR2 EPHB3 TGFBR1 |
BRAF, RAF1 (CRAF), TAO1 (TAOK1), MAP4K3, MAP3K5,
MAP3K14, MAP2K1 (MEK1), MAP2K2 (MEK2), MAP2K5, MAP2K7, MAPK1 (ERK2), MAPK10, RPS6KA1 (RSK1), RPS6KA3 (RSK2), RPS6KA4 (MSK2), DUSP21 PIK3CB, AKT2 AURKA, AURKC, BUB1, BUB1B, DDR2 EFNA3, EFNA5, EFNB3, EPHB1, EPHB4 ERBB3, TGFBR1 |
*Genes with common alternative names are in parentheses, and those related to the PI3K, MEK, or PDGFR pathways are in bold