1338320-94-7
Chemical Structure
Imofinostat
Synonym(s): ABT-301; MPT0E028; TMU-C-0012
- CAS No.: 1338320-94-7
- Formula:C17H16N2O4S
- Molecular Weight:344.38
IUPAC Name: (E)-N-hydroxy-3-(1-(phenylsulfonyl)indolin-5-yl)acrylamide
InChIKey: MGTIFSBCGGAZDB-VQHVLOKHSA-N
SMILES: O=C(/C=C/C1=CC2=C(C=C1)N(CC2)S(=O)(C3=CC=CC=C3)=O)NO
Biological Activity: Imofinostat (ABT-301; MPT0E028) is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. Imofinostat has a weak inhibitory effect on HDAC8 (IC50 of 2.5 μM), but no inhibitory effect on HDAC4 (IC50>10 μM). Imofinostat reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. Imofinostat has a broad-spectrum antitumor activity, including colorectal cancer, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and pancreatic cancer, while also showing therapeutic potential in non-tumor diseases like emphysema and pulmonary fibrosis[1][2][3][14][5][6].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Imofinostat | 99.40% | Imofinostat (ABT-301; MPT0E028) is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. Imofinostat has a weak inhibitory effect on HDAC8 (IC50 of 2.5 μM), but no inhibitory effect on HDAC4 (IC50>10 μM). Imofinostat reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. Imofinostat has a broad-spectrum antitumor activity, including colorectal cancer, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and pancreatic cancer, while also showing therapeutic potential in non-tumor diseases like emphysema and pulmonary fibrosis. | ||||||||||||||||||||
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References
- [1]. Huang HL, et al. Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo. PLoS One. 2012;7(8):e43645. [Content Brief]
- [2]. Huang HL, et al. Novel oral histone deacetylase inhibitor, MPT0E028, displays potent growth-inhibitory activity against human B-cell lymphoma in vitro and in vivo. Oncotarget. 2015 Mar 10;6(7):4976-91. [Content Brief]
- [3]. Chen MC, et al. The HDAC inhibitor, MPT0E028, enhances erlotinib-induced cell death in EGFR-TKI-resistant NSCLC cells. Cell Death Dis. 2013 Sep 19;4(9):e810. doi: 10.1038/cddis.2013.330. Erratum in: Cell Death Dis. 2024 Jul 9;15(7):490. [Content Brief]
- [5]. Liu CH, et al. MPT0E028, a novel pan-HDAC inhibitor, prevents pulmonary fibrosis through inhibition of TGF-β-induced CTGF expression in human lung fibroblasts: Involvement of MKP-1 activation. Eur J Pharmacol. 2024 Aug 15;977:176711. [Content Brief]
- [6]. Chao MW, et al. Combination treatment strategy for pancreatic cancer involving the novel HDAC inhibitor MPT0E028 with a MEK inhibitor beyond K-Ras status. Clin Epigenetics. 2019 May 29;11(1):85. [Content Brief]
