SIAIS178 is a potent BCR-ABL Degrader. SIAIS178 induces proper interaction between BCR-ABL and VHL ligase leading to effective degradation of BCR-ABL protein, achieves significant growth inhibition of BCR-ABL+ leukemic cells in vitro, and induces substantial tumor regression against K562 xenograft tumors in vivo. In addition, SIAIS178 also degrades several clinically relevant resistance-conferring mutations. Our data indicate that SIAIS178 as efficacious BCR-ABL degrader warrants extensive further investigation for the treatment of BCR-ABL+ leukemia.
MedKoo Cat#: 408033
Name: SIAIS178
CAS#: 2376047-73-1
Chemical Formula: C50H62ClN11O6S2
Exact Mass: 1011.4014
Molecular Weight: 1012.69
Elemental Analysis: C, 59.30; H, 6.17; Cl, 3.50; N, 15.21; O, 9.48; S, 6.33
The following data is based on the product molecular weight 1,012.69 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
