In vitro activity of CYT387 in 26 different hematopoietic and somatic cell lines
| Cell line . | Origin/phenotype . | Transforming kinase . | IC50, nM . |
|---|---|---|---|
| Ba/F3-EpoR parental control | Murine pre-B cell | IL-3–dependent growth | 1250 |
| Ba/F3-EpoR-JAK2-V617F | Murine pre-B cell | JAK2-V617F | 500 |
| 32D-EpoR parental | Murine myeloid precursor | IL-3–dependent growth | 1000 |
| 32D-EpoR-JAK2-WT | Murine myeloid precursor | IL-3–dependent growth | 1500 |
| 32D-EpoR-JAK2-V617F | Murine myeloid precursor | JAK2-V617F | 1500 |
| HEL | Acute myeloid leukemia | JAK2-V617F | 1500 |
| Ba/F3 | Murine pre-B cell | IL-3–dependent growth | 1750 |
| TF-1 | Acute myeloid leukemia | GM-CSF–dependent growth | 1250 |
| MO7e-p210 | Acute myeloid leukemia | BCR-ABL expression | 1500 |
| Ba/F3-p210 | Murine pre-B cell | BCR-ABL expression | 2000 |
| Ba/F3-p210-T315I | Murine pre-B cell | BCR-ABL expression | 1500 |
| 32D-p190 | Murine myeloid precursor | BCR-ABL expression | 1500 |
| KcL 22 | Chronic myeloid leukemia | BCR-ABL expression | 3000 |
| AR230-R1 | Chronic myeloid leukemia | BCR-ABL expression | 4000 |
| AR230-S | Chronic myeloid leukemia | BCR-ABL expression | > 5000 |
| KBM5 | Chronic myeloid leukemia | BCR-ABL expression | > 5000 |
| KU812 | Chronic myeloid leukemia | BCR-ABL expression | > 5000 |
| Lama | Chronic myeloid leukemia | BCR-ABL expression | > 5000 |
| Molm-14 | Acute myeloid leukemia | FLT3-ITD expression | 500 |
| CMK | Acute myeloid leukemia | JAK3-A572V | 1500 |
| REH | Acute lymphocytic leukemia | NN | 5000 |
| U266 | Multiple myeloma | IL-6–dependent growth | 750 |
| HeLa | Breast cancer | NN | 5000 |
| SKmI5 | Melanoma | NN | > 5000 |
| SKmI28 | Melanoma | NN | > 5000 |
| COS7 | Primate kidney | NN | > 5000 |
| Cell line . | Origin/phenotype . | Transforming kinase . | IC50, nM . |
|---|---|---|---|
| Ba/F3-EpoR parental control | Murine pre-B cell | IL-3–dependent growth | 1250 |
| Ba/F3-EpoR-JAK2-V617F | Murine pre-B cell | JAK2-V617F | 500 |
| 32D-EpoR parental | Murine myeloid precursor | IL-3–dependent growth | 1000 |
| 32D-EpoR-JAK2-WT | Murine myeloid precursor | IL-3–dependent growth | 1500 |
| 32D-EpoR-JAK2-V617F | Murine myeloid precursor | JAK2-V617F | 1500 |
| HEL | Acute myeloid leukemia | JAK2-V617F | 1500 |
| Ba/F3 | Murine pre-B cell | IL-3–dependent growth | 1750 |
| TF-1 | Acute myeloid leukemia | GM-CSF–dependent growth | 1250 |
| MO7e-p210 | Acute myeloid leukemia | BCR-ABL expression | 1500 |
| Ba/F3-p210 | Murine pre-B cell | BCR-ABL expression | 2000 |
| Ba/F3-p210-T315I | Murine pre-B cell | BCR-ABL expression | 1500 |
| 32D-p190 | Murine myeloid precursor | BCR-ABL expression | 1500 |
| KcL 22 | Chronic myeloid leukemia | BCR-ABL expression | 3000 |
| AR230-R1 | Chronic myeloid leukemia | BCR-ABL expression | 4000 |
| AR230-S | Chronic myeloid leukemia | BCR-ABL expression | > 5000 |
| KBM5 | Chronic myeloid leukemia | BCR-ABL expression | > 5000 |
| KU812 | Chronic myeloid leukemia | BCR-ABL expression | > 5000 |
| Lama | Chronic myeloid leukemia | BCR-ABL expression | > 5000 |
| Molm-14 | Acute myeloid leukemia | FLT3-ITD expression | 500 |
| CMK | Acute myeloid leukemia | JAK3-A572V | 1500 |
| REH | Acute lymphocytic leukemia | NN | 5000 |
| U266 | Multiple myeloma | IL-6–dependent growth | 750 |
| HeLa | Breast cancer | NN | 5000 |
| SKmI5 | Melanoma | NN | > 5000 |
| SKmI28 | Melanoma | NN | > 5000 |
| COS7 | Primate kidney | NN | > 5000 |
NN indicates not known; GM-CSF, granulocyte monocyte–colony stimulation factor; BCR-ABL, breakpoint cluster region–Abelson leukemia virus; and FLT3-ITD, Fms-like tyrosine kinase 3–insert tandem duplication.