| Description | Antifolate C2 (AGF 154) has antitumor activity with an IC of 0.14 nM measured in a growth inhibition assay of human tumor cells.Antifolate C2 can be used for the study of cancer and autoimmune diseases. |
| In vivo | Antifolate C2 （AGF154）作为潜在的抗肿瘤剂被合成。AGF154在表达叶酸受体（FRs）α或β（IC50s < 1 nM）或质子偶联叶酸运输器（PCFT）（IC50 < 7 nM）的中国地鼠卵巢（CHO）亚系中抑制细胞增殖。AGF154以亚纳摩尔浓度抑制人肿瘤细胞KB、IGROV1和SKOV3，反映了FRα和PCFT的摄取。AGF154抑制了甘氨酸酰胺核糖核酸甲酰转移酶（GARFTase）。在携带SKOV3肿瘤的严重联合免疫缺陷小鼠中，AGF154显示出效果。AGF154对PCFT以及FRα和β而非广泛表达的还原叶酸载体的选择性，为选择性肿瘤靶向提供了一个典范。 |
| Synonyms | AGF 154, AGF154, AGF-154 |
| molecular weight | 447.46 |
| Molecular formula | C19H21N5O6S |
| CAS | 1286279-90-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (122.92 mM) |
| References | 1. Wang L, et al. 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors. J Med Chem. 2015 Sep 10;58(17):6938-59. 2. Hou Z, et al. Dual Targeting of Epithelial Ovarian Cancer Via Folate Receptor α and the Proton-Coupled Folate Transporter with 6-Substituted Pyrrolo[2,3-d]pyrimidine Antifolates. Mol Cancer Ther. 2017 May;16(5):819-830. 3. Wilson M R, et al. Targeted therapy of non-small cell lung cancer (NSCLC) by novel 6-pyrrolo [2, 3-d] pyrimidine thienoyl antifolates with selective transport by the proton-coupled folate transporter (PCFT). Cancer Research.2015, 75(15_Supplement): 5403-5403. 4. Matherly LH, et al. Biology and therapeutic applications of the proton-coupled folate transporter. Expert Opin Drug Metab Toxicol. 2022 Oct;18(10):695-706. |