1361198-79-9
Chemical Structure
NEO212
- CAS No.: 1361198-79-9
- Formula:C17H20N6O4
- Molecular Weight:372.39
IUPAC Name: (S)-(4-(prop-1-en-2-yl)cyclohex-1-en-1-yl)methyl (3-methyl-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carbonyl)carbamate
InChIKey: MGTLGARADRIKNV-GFCCVEGCSA-N
SMILES: C(NC(OCC=1CC[C@H](C(C)=C)CC1)=O)(=O)C2=C3N(C=N2)C(=O)N(C)N=N3
Biological Activity: NEO212 is an orally active, blood-brain barrier permeable conjugate of Temozolomide (TMZ) (HY-17364) and Perillyl Alcohol (POH) (HY-N7000), with potent anticancer activity. NEO212 overcomes classical TMZ resistance and DNA alkylation by depleting MGMT. By inhibiting the FAK/Src signaling pathway, NEO212 reduces the production of MMP2 and MMP9, induces mesenchymal-epithelial transition, and inhibits the migration, invasion and tumor progression of glioma stem cells. NEO212 disrupts autophagy flux to enhance mitochondrial apoptosis; it induces differentiation of acute myeloid leukemia (AML) cells into macrophages and proliferation arrest[1][2][3][4].
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NEO212 | NEO212 is an orally active, blood-brain barrier permeable conjugate of Temozolomide (TMZ) (HY-17364) and Perillyl Alcohol (POH) (HY-N7000), with potent anticancer activity. NEO212 overcomes classical TMZ resistance and DNA alkylation by depleting MGMT. By inhibiting the FAK/Src signaling pathway, NEO212 reduces the production of MMP2 and MMP9, induces mesenchymal-epithelial transition, and inhibits the migration, invasion and tumor progression of glioma stem cells. NEO212 disrupts autophagy flux to enhance mitochondrial apoptosis; it induces differentiation of acute myeloid leukemia (AML) cells into macrophages and proliferation arrest. | |||||||||||||||||||||
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References
- [1]. Marín-Ramos NI, et al. NEO212 Inhibits Migration and Invasion of Glioma Stem Cells. Mol Cancer Ther. 2018;17(3):625-637. [Content Brief]
- [2]. Song X, et al. NEO212 induces mitochondrial apoptosis and impairs autophagy flux in ovarian cancer. J Exp Clin Cancer Res. 2019;38(1):239. Published 2019 Jun 7. [Content Brief]
- [3]. Chen TC, et al. Potent Therapeutic Activity of NEO212 in Preclinical Models of Human and Canine Leukaemia and Lymphoma. Vet Comp Oncol. 2025;23(3):412-423. [Content Brief]
- [4]. Chen TC, et al. NEO212, a Perillyl Alcohol-Temozolomide Conjugate, Triggers Macrophage Differentiation of Acute Myeloid Leukemia Cells and Blocks Their Tumorigenicity. Cancers (Basel). 2022;14(24):6065. Published 2022 Dec 9. [Content Brief]
