862505-00-8
Chemical Structure
Ralimetinib
Synonym(s): LY2228820
- CAS No.: 862505-00-8
- Formula:C24H29FN6
- Molecular Weight:420.53
IUPAC Name: 5-(2-(tert-butyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl)-3-neopentyl-3H-imidazo[4,5-b]pyridin-2-amine
InChIKey: XPPBBJCBDOEXDN-UHFFFAOYSA-N
SMILES: NC1=NC2=CC=C(C3=C(C4=CC=C(F)C=C4)N=C(C(C)(C)C)N3)N=C2N1CC(C)(C)C
Biological Activity: Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Ralimetinib | 98.58% | Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma. | ||||||||||||||||||||
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- [1]. Campbell RM, et al. Characterization of LY2228820 dimesylate, a potent and selective inhibitor of p38 MAPK with antitumor activity. Mol Cancer Ther. 2014;13(2):364-374. [Content Brief]
- [2]. Federspiel J, et al. p38 Mitogen-Activated Protein Kinase Inhibition of Mesenchymal Transdifferentiated Tumor Cells in Head and Neck Squamous Cell Carcinoma. Biomedicines. 2023;11(12):3301. Published 2023 Dec 13. [Content Brief]
Keywords
