| Bioactivity | Lefitolimod (MGN 1703) is a DNA-based TLR9 agonist and an immune surveillance reactivator. Lefitolimod induces HIV-specific immune responses and can be used for the research of cancer and HIV-1[1][4]. |
| Invitro | Lefitolimod (MGN 1703) 可能促进先天和适应性免疫反应，从而改善残余肿瘤的免疫介导控制[1]。Lefitolimod 靶向 TLR9 阳性的 pDCs，并触发其分泌 IFN-α 来激活先天免疫效应细胞，随后导致 IP-10 (一种趋化和血管静态蛋白) 的全身水平升高[2]。Lefitolimod (MGN1703) (1 μM; 48 h) 刺激细胞因子分泌 (干扰素 (IFN)-α、IFN-γ，白介素 (IL)-12、IL-6 和 IL-2)，并通过增加 CD80、CD40，人类白细胞抗原 (HLA)-DR 和 ICAM-1 的表达激活免疫细胞[3]。 |
| In Vivo | Lefitolimod (MGN1703) (2.5 and 60 μg/day; i.p.; daily for 7 days) 在小鼠血清中增加 IL-12p40 水平，无明显毒性[3]。 Animal Model: |
| Name | Lefitolimod |
| CAS | 1548439-51-5 |
| Sequence | DNA, cyclo[d(A-A-A-A-C-G-T-T-C-T-T-C-G-G-G-G-C-G-T-T-C-T-T-A-G-G-T-G-G-T-A-A-C-C-C-C-T-A-G-G-G-G-T-T-A-C-C-A-C-C-T-T-C-A-T-T-G-G-A-A-A-A-C-G-T-T-C-T-T-C-G-G-G-G-C-G-T-T-C-T-T-A-G-G-T-G-G-T-A-A-C-C-C-C-T-A-G-G-G-G-T-T-A-C-C-A-C-C-T-T-C-A-T-T-G-G)] |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Thomas M, et al. Immunotherapeutic maintenance treatment with toll-like receptor 9 agonist lefitolimod in patients with extensive-stage small-cell lung cancer: results from the exploratory, controlled, randomized, international phase II IMPULSE study. Ann Oncol. 2018 Oct 1;29(10):2076-2084. [2]. Jin Y, et al. Development of CpG oligodeoxynucleotide TLR9 agonists in anti-cancer therapy. Expert Rev Anticancer Ther. 2021 Aug;21(8):841-851. [3]. Schmidt M, et al. Design and Structural Requirements of the Potent and Safe TLR-9 Agonistic Immunomodulator MGN1703. Nucleic Acid Ther. 2015 Jun;25(3):130-40. [4]. McWhirter SM, et al. Nucleic Acid Sensors as Therapeutic Targets for Human Disease. Immunity. 2020 Jul 14;53(1):78-97. |