| Identification | Back Directory | [Name]
[(3R)-3-Amino-1-piperidinyl][2-[1-[(4-fluorophenyl)methyl]-1H-indol-2-yl]-3-methylimidazo[1,2-a]pyridin-7-yl]methanone | [CAS]
2308504-22-3 | [Synonyms]
JBI-589
(R)-(3-Aminopiperidin-1-yl)(2-(1-(4-fluorobenzyl)-1H-indol-2-yl)-3-methylimidazo[1,2-a]pyridin-7-yl)methanone
[(3R)-3-Amino-1-piperidinyl][2-[1-[(4-fluorophenyl)methyl]-1H-indol-2-yl]-3-methylimidazo[1,2-a]pyridin-7-yl]methanone | [Molecular Formula]
C29H28FN5O | [MOL File]
2308504-22-3.mol | [Molecular Weight]
481.57 |
| Chemical Properties | Back Directory | [density ]
1.33±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [solubility ]
Acetonitrile: Slightly Soluble: 0.1-1 mg/ml
DMSO: Slightly Soluble: 0.1-1 mg/ml | [form ]
Solid | [pka]
9.54±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
JBI-589 is a non-covalent PAD4 isoform-selective inhibitor with oral bioavailability. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors. JBI-589 can be used in cancer research[1][2]. | [in vivo]
JBI-589 (50 mg/kg, p.o., twice a day for 24 days) significantly inhibits the growth of primary tumors in LL2 and B16F10 tumor C57BL/6 mouse models[1]. | Animal Model: | LL2 tumor C57BL/6 mouse model; B16F10 tumor C57BL/6 mouse model | | Dosage: | 50 mg/kg | | Administration: | Oral gavage (p.o.), twice daily | | Result: | Led to a significant downregulation of CXCR2 receptor expression in Ly6G cells of the mice, while CXCR4 receptor expression remained unchanged.
Had no effect on the cell counts of bone marrow cells, CD8 T cells, and NK cells in tumor-bearing mice model. |
| [References]
[1] Deng H, et al. A Novel Selective Inhibitor JBI-589 Targets PAD4-Mediated Neutrophil Migration to Suppress Tumor Progression. Cancer Res. 2022 Oct 4;82(19):3561-3572. DOI:10.1158/0008-5472.CAN-21-4045
[2] Gajendran C, et al. Alleviation of arthritis through prevention of neutrophil extracellular traps by an orally available inhibitor of protein arginine deiminase 4. Sci Rep. 2023 Feb 23;13(1):3189. DOI:10.1038/s41598-023-30246-2 |
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| Company Name: |
BIO- S
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| Tel: |
19143500486 |
| Website: |
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| Company Name: |
Biorbyt Ltd.
|
| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
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