Table 1. Activity of melflufen in various in vitro models of MM.
| Cell designation | Cell line characteristics and reference | Sensitivity* to melflufen IC50 µM and reference |
|---|---|---|
| RPMI-8226 | Sensitive maternal line (Moore 1968) Melphalan IC50 > 10 µM (Chauhan, Ray et al. 2013) |
1.0 [16] 1.6 [20] |
| 8226LR5 | Subline of RPMI-8226, resistant to melphalan (Bellamy 1991) Melphalan IC50 > 10 µM (Chauhan, Ray et al. 2013) |
2.6 [16] 4.5 [20] |
| 8226Dox40 | Subline of RPMI-8226, resistant to doxorubicin, mitoxantrone, acronycine, etoposide, and vincristine Sensitive to melphalan and dexamethasone (Dalton 1986) |
1.8 [16] <0.5 [20] |
| INA-6 | Dependent on IL-6 for growth (Burger 1998) | <0.5 [20] |
| ARP-1 | Sensitive to dexamethasone | 1.7 [20] |
| MM.1S | Sensitive to dexamethasone (Goldman-Leikin 1989, Moalli 1992) | <0.5 [20] |
| MM.1R | Resistant to dexamethasone (Goldman-Leikin 1989, Moalli 1992) | <0.5[20] |
| ANBL-6.WT | Bortezomib sensitive Melphalan IC50 5.2 µM (Chauhan, Ray et al. 2013) |
0.41 [20] |
| ANBL-6.BR | Bortezomib resistant Melphalan IC50 >10 µM (Chauhan, Ray et al. 2013) |
0.81[20] |
| Primary cultures of human myeloma cells | Melphalan IC50 10 µM (Wickstrom, Haglund et al. 2008) |
0.2 µM [32] |
*The sensitivity has been estimated with fluorometric microculture cytotoxicity assay (Gullbo 2003 [16] and Wickstrom 2008 [32]) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay (Chauhan 2013 [20]). Survival-concentration bar graphs in Chauhan 2013 were re-analyzed to get the IC50-values presented.