1799328-50-9
Chemical Structure
Tolinapant dihydrochloride
Synonym(s): ASTX660 dihydrochloride
- CAS No.: 1799328-50-9
- Formula:C30H44Cl2FN5O3
- Molecular Weight:612.61
IUPAC Name: 1-(6-(4-fluorobenzyl)-5-(hydroxymethyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)-2-((2R,5R)-5-methyl-2-(((R)-3-methylmorpholino)methyl)piperazin-1-yl)ethan-1-one dihydrochloride
InChIKey: BZXQBXXYGJSOTM-FBLZNNLISA-N
SMILES: C[C@H](COCC1)N1C[C@@H](CN[C@H](C)C2)N2CC(N3C4=CC(CC5=CC=C(F)C=C5)=C(CO)N=C4C(C)(C)C3)=O.Cl.Cl
Biological Activity: Tolinapant dihydrochloride (ASTX660 dihydrochloride) is an orally active cIAP1/2 and XIAP antagonist, with an IC50 of < 40 nM against XIAP and an IC50 of <12 nM against cIAP1. Tolinapant dihydrochloride triggers TNFα-dependent Apoptosis in cancer cells. Tolinapant dihydrochloride inhibits tumor growth in mouse xenograft models. Tolinapant dihydrochloride can be used in research related to breast cancer, melanoma, lymphoma, multiple myeloma, acute lymphoblastic leukemia and advanced solid tumors[1][2][3][4][5].
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Tolinapant dihydrochloride | Tolinapant dihydrochloride (ASTX660 dihydrochloride) is an orally active cIAP1/2 and XIAP antagonist, with an IC50 of < 40 nM against XIAP and an IC50 of <12 nM against cIAP1. Tolinapant dihydrochloride triggers TNFα-dependent Apoptosis in cancer cells. Tolinapant dihydrochloride inhibits tumor growth in mouse xenograft models. Tolinapant dihydrochloride can be used in research related to breast cancer, melanoma, lymphoma, multiple myeloma, acute lymphoblastic leukemia and advanced solid tumors. | |||||||||||||||||||||
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- [1]. Ward GA, et al. ASTX660, a Novel Non-peptidomimetic Antagonist of cIAP1/2 and XIAP, Potently Induces TNFα-Dependent Apoptosis in Cancer Cell Lines and Inhibits Tumor Growth. Molecular cancer therapeutics. 2018 Jul;17(7):1381-1391. [Content Brief]
- [2]. Martins V, et al. The preclinical pharmacokinetics of Tolinapant-A dual cIAP1/XIAP antagonist with in vivo efficacy. Pharmacology research & perspectives. 2024 Dec;12(6):e70030. [Content Brief]
- [3]. Smyth T, et al. The dual IAP antagonist, ASTX660, increases the anti-tumor activity of paclitaxel in preclinical models of triple-negative breast cancer in vivo[J]. Cancer Research, 2016, 76(14_Supplement): 1287-1287.
- [4]. Tazuru K, et al. The IAP antagonist tolinapant enhances the anti-tumor activity of cell therapies. European journal of pharmacology. 2025 May 15;995:177400. [Content Brief]
- [5]. Mita MM, et al. A Phase I Study of ASTX660, an Antagonist of Inhibitors of Apoptosis Proteins, in Adults with Advanced Cancers or Lymphoma. Clinical cancer research : an official journal of the American Association for Cancer Research. 2020 Jun 15;26(12):2819-2826. [Content Brief]
Keywords
