Rebastinib (DCC-2036) is a potent, orally bioavailable tyrosine kinase inhibitor that primarily targets the ABL1 kinase, including the T315I gatekeeper mutation associated with resistance to first- and second-generation BCR-ABL inhibitors. It exhibits nanomolar potency, with reported IC₅₀ values of approximately 0.8 nM against wild-type BCR-ABL and 4 nM against the T315I mutant in enzymatic assays. Rebastinib also inhibits other kinases such as Tie2 (TEK), with an IC₅₀ of ~1.2 nM, implicating additional anti-angiogenic and anti-metastatic potential. In cellular assays, rebastinib demonstrates sub-nanomolar to low nanomolar activity against BCR-ABL–expressing leukemia cells, including those harboring the T315I mutation, with corresponding inhibition of downstream signaling (e.g., STAT5 phosphorylation). Preclinical studies show significant tumor regression and prolonged survival in mouse xenograft models of chronic myeloid leukemia (CML) and solid tumors.
MedKoo Cat#: 581303
Name: Rebastinib tosylate
CAS#: 1033893-29-6 (tosylate)
Chemical Formula: C37H36FN7O6S
Exact Mass: 725.2432
Molecular Weight: 725.80
Elemental Analysis: C, 61.23; H, 5.00; F, 2.62; N, 13.51; O, 13.23; S, 4.42
The following data is based on the product molecular weight 725.80 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 |
