1033893-29-6
Chemical Structure
Rebastinib tosylate
Synonym(s): DCC-2036 tosylate
- CAS No.: 1033893-29-6
- Formula:C37H36FN7O6S
- Molecular Weight:725.79
IUPAC Name: 4-(4-(3-(3-(tert-butyl)-1-(quinolin-6-yl)-1H-pyrazol-5-yl)ureido)-3-fluorophenoxy)-N-methylpicolinamide 4-methylbenzenesulfonate
InChIKey: ARPBZBAWXAVDCE-UHFFFAOYSA-N
SMILES: O=C(NC1=CC(C(C)(C)C)=NN1C2=CC3=CC=CN=C3C=C2)NC4=CC=C(C=C4F)OC5=CC(C(NC)=O)=NC=C5.O=S(O)(C6=CC=C(C)C=C6)=O
Biological Activity: Rebastinib tosylate (DCC-2036 tosylate) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC50 values of 0.8 nM and 4 nM against Abl1WT and Abl1T315I, respectively. Rebastinib tosylate potently inhibits CYP2C8 (IC50 = 0.0533 μM) and CYP2C9 (IC50 = 2.54 μM). Rebastinib tosylate allosterically inhibits Tie2 with an IC50 of 0.63 nM. Rebastinib tosylate inhibits the transcriptional activity of FoxO1. Rebastinib tosylate inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib tosylate induces Apoptosis. Rebastinib tosylate exerts anti-tumor activity in breast cancer. Rebastinib tosylate exerts anti-angiogenic effects. Rebastinib tosylate increases myotube diameter and improves reduced contractility. Rebastinib tosylate can be used in research related to triple-negative breast cancer, luminal breast cancer, pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia[1][2][3][4].
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Rebastinib tosylate | Rebastinib tosylate (DCC-2036 tosylate) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC50 values of 0.8 nM and 4 nM against Abl1WT and Abl1T315I, respectively. Rebastinib tosylate potently inhibits CYP2C8 (IC50 = 0.0533 μM) and CYP2C9 (IC50 = 2.54 μM). Rebastinib tosylate allosterically inhibits Tie2 with an IC50 of 0.63 nM. Rebastinib tosylate inhibits the transcriptional activity of FoxO1. Rebastinib tosylate inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib tosylate induces Apoptosis. Rebastinib tosylate exerts anti-tumor activity in breast cancer. Rebastinib tosylate exerts anti-angiogenic effects. Rebastinib tosylate increases myotube diameter and improves reduced contractility. Rebastinib tosylate can be used in research related to triple-negative breast cancer, luminal breast cancer, pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia. | |||||||||||||||||||||
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- [1]. Feng K, et al. The Suppressive Effect of Rebastinib on Triple-negative Breast Cancer Tumors Involves Multiple Mechanisms of Action. Anticancer research. 2023 Jun;43(6):2609-2624. [Content Brief]
- [2]. Harney AS, et al. The Selective Tie2 Inhibitor Rebastinib Blocks Recruitment and Function of Tie2 Macrophages in Breast Cancer and Pancreatic Neuroendocrine Tumors. Molecular cancer therapeutics. 2017 Nov;16(11):2486-2501. [Content Brief]
- [3]. Sato T, et al. Rebastinib inhibits FoxO1 activity and reduces dexamethasone-induced atrophy and its-related gene expression in cultured myotubes. The journal of physiological sciences : JPS. 2025 Mar;75(1):100012. [Content Brief]
- [4]. Chan WW, et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer cell. 2011 Apr 12;19(4):556-68. [Content Brief]
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