他匹莫德
他匹莫德 性质
| 沸点 | 658.0±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.29 |
| 储存条件 | Desiccate at +4°C |
| 溶解度 | 可溶于DMSO |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 6.52±0.70(Predicted) |
| 颜色 | 粉红至红色 |
| InChIKey | ZMELOYOKMZBMRB-DLBZAZTESA-N |
| SMILES | O=C(C(C1=CN(C2=C1C=C(C(Cl)=C2)C(N3[C@@H](CN([C@H](C3)C)CC4=CC=C(C=C4)F)C)=O)C)=O)N(C)C |
他匹莫德 用途与合成方法
|
p38α 9 nM (IC 50 ) |
p38β 90 nM (IC 50 ) |
Talmapimod (SCIO-469) (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells.
Talmapimod inhibits LPS-induced TNF-a production in human whole blood.
Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells.
Western Blot Analysis
| Cell Line: | MM.1S, U266, RPMI8226, MM.1R, and RPMI-Dox40 cell lines |
| Concentration: | 100, 200 nM |
| Incubation Time: | 1 hour |
| Result: | Strongly inhibits phosphorylation of p38 MAPK. |
Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease.
Talmapimod inhibits multiple myeloma growth and prevents bone disease in the 5T2MM and 5T33MM models.
Talmapimod (10-90 mg/kg; p.o.; twice daily orally for 14 days) dose-dependently reduced tumor growth and also dose-dependently reduced weight of the palpable tumors at termination.
| Animal Model: | Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors) |
| Dosage: | P.o.; twice daily orally for 14 days |
| Administration: | 10, 30, 90 mg/kg |
| Result: | Dose-dependently reduced tumor growth. |
他匹莫德 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025-12-22 | HY-10406 | 他匹莫德 | 309913-83-5 | 1 mg | 550 |
| 2025-12-22 | HY-10406 | 他匹莫德 | 309913-83-5 | 2mg | 810 |