| Bioactivity | SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 TFA can be used to research chronic myeloid leukemia (CML)[1]. |
| Invitro | SIAIS100 对 K562 细胞具有抗增殖活性，IC50 值为 12 nM[1]。SIAIS100 剂量为 5 nM 和 100 nM 时对 BCR-ABL 的降解率分别为 81.78% 和 91.20%[1]。SIAIS100 (100 nM; 8 h) 显著降低 K562 细胞的 BCR-ABL[1]。SIAIS100 (100 nM; 6 h) 持续且强烈地 BCR-ABL 降解，并在药物去除后保持持久的细胞反应[1]。SIAIS100 (1-1000 nM) 显著降低了突变体 G250E/T315I，且具有剂量依赖性，同时在 32D 细胞中抑制了 BCR-ABL 信号 （通过 p-BCR-ABL 水平评估）[1]。 |
| Name | SIAIS100 TFA |
| Formula | C46H51ClF5N9O7S |
| Molar Mass | 1004.46 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, stored under nitrogen, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture) |
| Reference | [1]. Liu H, et al. Discovery and characterization of novel potent BCR-ABL degraders by conjugating allosteric inhibitor. Eur J Med Chem. 2022 Dec 15;244:114810. |