他匹莫德
| 中文名稱 | 他匹莫德 |
|---|---|
| 中文同義詞 | 6-氯-5-[[(2R,5S)-4-[(4-氟苯基)甲基]-2,5-二甲基-1-哌嗪基]甲?；鵠-N,N,1-三甲基-ALPHA-氧代-1H-吲哚-3-乙酰胺;他匹莫德;P38抑制劑(SCIO-469);他匹莫德,10 MM DMSO 溶液;Talmapimod (他匹莫德);SCIO-469 (Talmapimod;SCIO469;SCIO 469);化合物:Talmapimod (SCIO-469);化合物：Talmapimod (SCIO-469) |
| 英文名稱 | talmapimod |
| 英文同義詞 | talmapimod;6-Chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-alpha-oxo-1H-indole-3-acetamide;Unii-B1E00kq6nt;6-Chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo-1H-Indole-3-acetamidehydrochloride;SCIO 469 hydrochloride;6-Chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)Methyl]-2,5-diMethyl-1-piperazinyl]carbonyl]-N,N,1-triMethyl-α-oxo-1H-indole-3-acetaMide;SCIO 469;Scios 469 |
| CAS號 | 309913-83-5 |
| 分子式 | C27H30ClFN4O3 |
| 分子量 | 513 |
| EINECS號 | |
| 相關(guān)類別 | 細胞生物學(xué)試劑 |
| Mol文件 | 309913-83-5.mol |
| 結(jié)構(gòu)式 |  |
他匹莫德 性質(zhì)
| 沸點 | 658.0±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.29 |
| 儲存條件 | Desiccate at +4°C |
| 溶解度 | 可溶于DMSO |
| 形態(tài) | 結(jié)晶固體 |
| 酸度系數(shù)(pKa) | 6.52±0.70(Predicted) |
| 顏色 | 粉紅至紅色 |
| 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 |
|
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. |
安全信息
| WGK Germany | WGK 3 |
|---|---|
| 海關(guān)編碼 | 2924297099 |
| 存儲類別 | 11 - 可燃固體 |
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-10406 | 他匹莫德 Talmapimod | 309913-83-5 | 1 mg | 550元 |
| 2026/06/05 | HY-10406 | 他匹莫德 Talmapimod | 309913-83-5 | 2mg | 810元 |