他匹莫德
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- CAS号:
- 309913-83-5
- 英文名:
- talmapimod
- 英文别名:
- SCIO 469;Scios 469;talmapimod;Unii-B1E00kq6nt;TalMapiMod (SCIO-469);SCIO 469 - Talmapimod;SCIO 469 hydrochloride;Talmapimod hydrochloride;TALMAPIMOD;SCIO469;SCIO 469;cytotoxicity,multiple,inhibit,tumor,SCIO 469,SCIO469,cells,Hsp27,Inhibitor,phosphorylation,Talmapimod,p38 MAPK,myeloma
- 中文名:
- 他匹莫德
- 中文别名:
- 他匹莫德;P38抑制剂(SCIO-469);6-氯-5-[[(2R,5S)-4-[(4-氟苯基)甲基]-2,5-二甲基-1-哌嗪基]甲酰基]-N,N,1-三甲基-ALPHA-氧代-1H-吲哚-3-乙酰胺
- CBNumber:
- CB81518535
- 分子式:
- C27H30ClFN4O3
- 分子量:
- 513
- MOL File:
- 309913-83-5.mol
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他匹莫德化学性质
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沸点:
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658.0±65.0 °C(Predicted)
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密度:
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1.29
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储存条件:
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Desiccate at +4°C
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溶解度:
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DMSO: soluble
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形态:
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A crystalline solid
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酸度系数(pKa):
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6.52±0.70(Predicted)
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他匹莫德性质、用途与生产工艺
Talmapimod (他匹莫德; SCIO-469) 是 p38α 选择性的，具有口服活性的，ATP 竞争性的抑制剂，IC50 值是 9 nM，约为 p38β 的10倍，在 20 个其他激酶 (包括其他 MAPKs) 上显示出至少 2000 倍的选择性。
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p38α
9 nM (IC
50
)
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p38β
90 nM (IC
50
)
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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
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Cell Line:
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MM.1S, U266, RPMI8226, MM.1R, and RPMI-Dox40 cell lines
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Concentration:
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100, 200 nM
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Incubation Time:
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1 hour
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Result:
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Strongly inhibits phosphorylation of p38 MAPK.
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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.
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Animal Model:
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Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors)
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Dosage:
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P.o.; twice daily orally for 14 days
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Administration:
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10, 30, 90 mg/kg
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Result:
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Dose-dependently reduced tumor growth.
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他匹莫德
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-10406 | Talmapimod | | 1 mg | 623元 |
| 2024/04/30 | HY-10406 | 他匹莫德
Talmapimod | 309913-83-5 | 2mg | 900元 |
他匹莫德
生产厂家
全球有 72家供应商
他匹莫德国内生产厂家
309913-83-5, 他匹莫德 相关搜索:
- 细胞生物学试剂
- C27H30ClFN4O3HCl
- C27H30ClFN4O3
- P38抑制剂(SCIO-469)
- 他匹莫德
- 6-氯-5-[[(2R,5S)-4-[(4-氟苯基)甲基]-2,5-二甲基-1-哌嗪基]甲酰基]-N,N,1-三甲基-ALPHA-氧代-1H-吲哚-3-乙酰胺
- 309913-83-5
- cytotoxicity,multiple,inhibit,tumor,SCIO 469,SCIO469,cells,Hsp27,Inhibitor,phosphorylation,Talmapimod,p38 MAPK,myeloma
- 1H-Indole-3-acetamide, 6-chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo-
- SCIO 469 - Talmapimod
- TALMAPIMOD;SCIO469;SCIO 469
- Talmapimod hydrochloride
- TalMapiMod (SCIO-469)
- Scios 469
- SCIO 469
- 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 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-acetamidehydrochloride
- Unii-B1E00kq6nt
- 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
- talmapimod