1710768-30-1
Chemical Structure
Ibrutinib-MPEA
- CAS No.: 1710768-30-1
- Formula:C32H39N9O2
- Molecular Weight:581.71
IUPAC Name: (R,E)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-4-(4-(2-aminoethyl)piperazin-1-yl)but-2-en-1-one
InChIKey: RQQVGXHWCJBNPV-DSCGJTOLSA-N
SMILES: NCCN1CCN(C/C=C/C(N2C[C@H](N3N=C(C4=CC=C(OC5=CC=CC=C5)C=C4)C6=C(N)N=CN=C63)CCC2)=O)CC1
Biological Activity: Ibrutinib-MPEA is an orally active, blood-brain barrier permeable inhibitor of BTK and STAT5. As a derivative of Ibrutinib (HY-10997) conjugated with a PROTAC linker, Ibrutinib-MPEA allows the synthesis of a series of PROTAC molecules. Ibrutinib-MPEA significantly reduces the proliferation of neoplastic mast cells and primary mastocytoma cells by inducing apoptosis and inhibiting IgE-dependent histamine release. Ibrutinib-MPEA is applicable to the research of canine mast cell tumors, cerebral ischemia/reperfusion injury in diabetic mice, and neuroinflammation-related diseases[1][2][3].
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Ibrutinib-MPEA | 99.71% | Ibrutinib-MPEA is an orally active, blood-brain barrier permeable inhibitor of BTK and STAT5. As a derivative of Ibrutinib (HY-10997) conjugated with a PROTAC linker, Ibrutinib-MPEA allows the synthesis of a series of PROTAC molecules. Ibrutinib-MPEA significantly reduces the proliferation of neoplastic mast cells and primary mastocytoma cells by inducing apoptosis and inhibiting IgE-dependent histamine release. Ibrutinib-MPEA is applicable to the research of canine mast cell tumors, cerebral ischemia/reperfusion injury in diabetic mice, and neuroinflammation-related diseases. | ||||||||||||||||||||
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- [1]. Gamperl S, et al. Effects of ibrutinib on proliferation and histamine release in canine neoplastic mast cells. Vet Comp Oncol. 2019;17(4):553-561. [Content Brief]
- [2]. Jin L, et al. Ibrutinib ameliorates cerebral ischemia/reperfusion injury through autophagy activation and PI3K/Akt/mTOR signaling pathway in diabetic mice. Bioengineered. 2021;12(1):7432-7445. [Content Brief]
- [3]. Nam HY, et al. Ibrutinib suppresses LPS-induced neuroinflammatory responses in BV2 microglial cells and wild-type mice. J Neuroinflammation. 2018;15(1):271. Published 2018 Sep 19. [Content Brief]
Keywords
