1964516-64-0
Chemical Structure
NCI-006
- CAS No.: 1964516-64-0
- Formula:C31H24F2N4O4S3
- Molecular Weight:650.74
SMILES: O=C(C1=CSC(N2N=C(C(CC3=CC=C(S(=O)(N)=O)C(F)=C3)=C2CC4CC4)C5=CC(C#CC6=CC=C(C)S6)=C(F)C=C5)=N1)O
Biological Activity: NCI-006 is an orally active lactate dehydrogenase (LDH) inhibitor (LDHA IC50 = 0.06 μM; LDHB IC50 = 0.03 μM). NCI-006 inhibits intratumoral LDH activity, lactate production, and tumor growth in a mouse pancreatic cancer model. NCI-006 inhibits glycolysis and induces apoptosis in vitro. NCI-006 enhances the radiosensitivity of glycolytic tumor cell lines while sparing non-glycolytic/normal cells (1522, skin fibroblasts) in combination with ionizing radiation (IR). NCI-006 exhibits synergistic antitumor effects in combination with IACS-010759 (HY-112037) against colorectal and gastric cancers. NCI-006 targets glycolysis by inhibiting lactate dehydrogenase impairs tumor growth in an Ewing sarcoma model[1][2][3][4][5][6][7].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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NCI-006 | 98.73% | NCI-006 is an orally active lactate dehydrogenase (LDH) inhibitor (LDHA IC50 = 0.06 μM; LDHB IC50 = 0.03 μM). NCI-006 inhibits intratumoral LDH activity, lactate production, and tumor growth in a mouse pancreatic cancer model. NCI-006 inhibits glycolysis and induces apoptosis in vitro. NCI-006 enhances the radiosensitivity of glycolytic tumor cell lines while sparing non-glycolytic/normal cells (1522, skin fibroblasts) in combination with ionizing radiation (IR). NCI-006 exhibits synergistic antitumor effects in combination with IACS-010759 (HY-112037) against colorectal and gastric cancers. NCI-006 targets glycolysis by inhibiting lactate dehydrogenase impairs tumor growth in an Ewing sarcoma model. | ||||||||||||||||||||
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References
- [1]. Nobu Oshima, et al. Abstract 6222: Comprehensive monitoring of pyruvate metabolism in cancer cells and tumors reveals vulnerability to metabolic inhibition therapy with small molecules. Cancer Res 15 June 2022; 82 (12_Supplement): 6222.
- [2]. Nobu Oshima, et al. Abstract 2783: Monitoring of a novel LDH inhibitor and mitochondrial inhibitor efficacy in vivo in a glycolytic pancreatic cancer model using hyperpolarized13C MRI. Cancer Res 15 August 2020; 80 (16_Supplement): 2783.
- [3]. Oshima N, et al. Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy. Cell Rep. 2020 Feb 11;30(6):1798-1810.e4. [Content Brief]
- [4]. Rai G, et al. Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH). J Med Chem. 2017 Nov 22;60(22):9184-9204. [Content Brief]
- [5]. Suchet Taori, et al. Abstract 3587: Targeting cancer metabolism: A novel approach for improved radiotherapy. Cancer Res 1 July 2019; 79 (13_Supplement): 3587.
- [6]. Aisu Y, et al. Dual inhibition of oxidative phosphorylation and glycolysis exerts a synergistic antitumor effect on colorectal and gastric cancer by creating energy depletion and preventing metabolic switch. PLoS One. 2024 Dec 12;19(12):e0309700. [Content Brief]
- [7]. Yeung C, et al. Targeting Glycolysis through Inhibition of Lactate Dehydrogenase Impairs Tumor Growth in Preclinical Models of Ewing Sarcoma. Cancer Res. 2019 Oct 1;79(19):5060-5073. [Content Brief]
