Tagraxofusp (SL-401) 是一种有效的IL-3受体抑制剂，可抑制多发性骨髓瘤 (MM) 骨髓 (BM) 微环境中浆细胞样树突状细胞 (pDCs) 的生长。Tagraxofusp 与 Bortezomib (HY-10227)、Pomalidomide (HY-10984) 有协同抑制多发性骨髓瘤的作用。
| 生物活性 | Tagraxofusp (SL-401) is a potentIL-3receptorinhibitor to inhibits plasmacytoid dendritic cells (pDCs) growth in multiple myeloma (MM) bone marrow (BM) microenvironment. Tagraxofusp has synergistic effect withBortezomib(HY-10227) andPomalidomide(HY-10984) to suppress multiple myeloma (MM)[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | Tagraxofusp (0-1367 pM; 72 h) inhibits pDCs viability, as well as pDC-induced proliferation of MM cells.
Tagraxofusp (0-136.7 pM; 2-3 weeks) inhibits osteoclast formation and bone resorption, as well as stabilizes osteoblast formation[1].
Tagraxofusp (0-13.67 nM; 48 h) targets tumor-initiating stem-like cells in MM[1].
Cell Viability Assay[1] | Cell Line: | Cancer stem-like cells in MM | | Concentration: | 0 nM, 0.013 nM, 0.13 nM, 1.3 nM, 13.67 nM | | Incubation Time: | 48 hours | | Result: | Inhibits cancer stem-like cells with s of 30 pM (pDCs), 50 nM (MM-SP-Oct4 cells), 75 pM (RPMI-8226-Oct4 cells), 350 pM (MM-SP cells), and 1367 pM (RPMI-8226 cells), respectively. |
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体内研究
(In Vivo) | Tagraxofusp (12-50 μg/kg; i.v.; 5 times per week for 3 weeks) blocks pDC-induced tumor growth and prolongs SCID-hu mice survival in subcutaneous INA-6 MM xenograft model[1].
Tagraxofusp (16 μg/kg; i.v.; 5 times per week for 1 weeks) enhances the anti-MM activity of 2.5 mg/kgPomalidomidein CB-17 mice of subcutaneous MM xenograft model[1].
| Animal Model: | SCID-hu mice with INA-6 MM cells[1] | | Dosage: | 12 μg/kg, 16 μg/kg, 25 μg/kg and 50 μg/kg | | Administration: | Intravenous injection; for 5 consecutive days each week for 3 weeks | | Result: | Blocked pDC-induced tumor growth and prolonged mice survival at 12 μg/kg.
Showed well tolerance at 16 μg/kg, while higher doses resulted in body weight decrease and toxicity. |
| Animal Model: | CB-17 mice with subcutaneous MM xenograft model[1] | | Dosage: | 16 μg/kg; with or without 2.5 mg/kg Pomalidomide (p.o.; 4 consecutive days weekly for 2 weeks) | | Administration: | Intravenous injection; dose at 5 consecutive days for first week | | Result: | Enhanced the anti-MM activity of proteasome inhibitor and immunomodulatory drug pomalidomide. |
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| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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