IC50 values for HG-7-85-01
| Cell line . | HG-7-85-01, nM . |
|---|---|
| Ba/F3 | 2410 |
| Bcr-Abl* | |
| Ba/F3.p210 | 58.5 |
| Ba/F3-T315I | 140 |
| Ba/F3-Y253H | 500-< 1000 |
| Ba/F3-E255K | 500-< 1000 |
| Ba/F3-Q252H | 50-< 100 |
| Ba/F3-V289L | 500-< 1000 |
| Ba/F3-E292K | 500-< 1000 |
| Ba/F3-Y253C | < 100 |
| Ba/F3-M351T | 250-500 |
| Ba/F3-F317L | 500-1000 |
| Ba/F3-F486S | 500 |
| KIT* | |
| Ba/F3-insAY | > 1000 |
| Ba/F3-insAY+V654A | > 1000 |
| Ba/F3-insAY+T670I | ≥ 1000 |
| Ba/F3-V559D | 250-500 |
| Ba/F3-delWK | 12.5-25 |
| Ba/F3-delWK+V654A | 25-50 |
| Ba/F3-delWK+T670I | 25-50 |
| Ba/F3-delWK+Y823D | 500-1000 |
| Ba/F3-T670I | 250 |
| PDGFR* | |
| Ba/F3-TEL/PDGFRβ | < 100 |
| Ba/F3-PDGFRβ-T681I | > 1000 |
| Ba/F3-PDGFRα-T674M | 6.25 |
| Ba/F3-PDGFRα-T674I | 6.25 |
| Ba/F3-PDGFRα-D842V | 1000 |
| Ba/F3-PDGFRα-V561D | > 1000 |
| Cell line . | HG-7-85-01, nM . |
|---|---|
| Ba/F3 | 2410 |
| Bcr-Abl* | |
| Ba/F3.p210 | 58.5 |
| Ba/F3-T315I | 140 |
| Ba/F3-Y253H | 500-< 1000 |
| Ba/F3-E255K | 500-< 1000 |
| Ba/F3-Q252H | 50-< 100 |
| Ba/F3-V289L | 500-< 1000 |
| Ba/F3-E292K | 500-< 1000 |
| Ba/F3-Y253C | < 100 |
| Ba/F3-M351T | 250-500 |
| Ba/F3-F317L | 500-1000 |
| Ba/F3-F486S | 500 |
| KIT* | |
| Ba/F3-insAY | > 1000 |
| Ba/F3-insAY+V654A | > 1000 |
| Ba/F3-insAY+T670I | ≥ 1000 |
| Ba/F3-V559D | 250-500 |
| Ba/F3-delWK | 12.5-25 |
| Ba/F3-delWK+V654A | 25-50 |
| Ba/F3-delWK+T670I | 25-50 |
| Ba/F3-delWK+Y823D | 500-1000 |
| Ba/F3-T670I | 250 |
| PDGFR* | |
| Ba/F3-TEL/PDGFRβ | < 100 |
| Ba/F3-PDGFRβ-T681I | > 1000 |
| Ba/F3-PDGFRα-T674M | 6.25 |
| Ba/F3-PDGFRα-T674I | 6.25 |
| Ba/F3-PDGFRα-D842V | 1000 |
| Ba/F3-PDGFRα-V561D | > 1000 |
Relative IC50 ranges for HG-85-01 in BCR-ABL-, Kit-, and PDGFR-expressing cell lines.
All cellular proliferation assays performed were 2.5 to 3 days in duration, except for PDGFRα-D842V and PDGFRα-V561D, which were 2-day experiments.