| Identification | Back Directory | [Name]
talmapimod | [CAS]
309913-83-5 | [Synonyms]
SCIO 469
Scios 469
talmapimod
Unii-B1E00kq6nt
SCIO 469 - Talmapimod
TalMapiMod (SCIO-469)
SCIO 469 hydrochloride
Talmapimod hydrochloride
TALMAPIMOD;SCIO469;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
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-
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
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 | [Molecular Formula]
C27H30ClFN4O3 | [MDL Number]
MFCD11973651 | [MOL File]
309913-83-5.mol | [Molecular Weight]
513 |
| Chemical Properties | Back Directory | [Boiling point ]
658.0±65.0 °C(Predicted) | [density ]
1.29 | [storage temp. ]
Desiccate at +4°C | [solubility ]
DMSO: soluble | [form ]
A crystalline solid | [pka]
6.52±0.70(Predicted) | [color ]
Pink to red | [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 |
| Hazard Information | Back Directory | [Uses]
Talmapimod is a p38 mitogen-activated protein (MAP) kinase inhibitor. Talmapimod reduced human myeloma cell growth in vivo both at early and advanced phases of the disease in mouse xenograft models. T
almapimod that blocks tumor necrosis factor-α, interleukin-1β, and cyclooxygenase-2 synthesis in patients with active rheumatoid arthritis (RA) | [Definition]
ChEBI: An indolecarboxamide obtained by formal condensation of the carboxy group of 6-chloro-3-[(dimethylamino)(oxo)acetyl]-1-methylindole-5-carboxylic acid with the secondary amino group of (2S,5R)-1-[(4-fluorophenyl)methyl]-2,
-dimethylpiperazine. It is a potent inhibitor of MAPK and exhibits anti-cancer properties. | [Biological Activity]
SCIO-469 (Talmapimod) is an orally activepotent and selective mitogen-activated protein kinase (MAPK) p38alpha (p38αMAPK14) inhibitor (IC50 = 9 nM; 10-fold over p38β>2000-fold over 20 other kinases) with no significant affinity toward a panel of 70 enzymes and receptors. SCIO-469 inhibits multiple myeloma (MM) growth in mice in vivo (150 or 450 mg/kg powder diet; 5T2MM and 5T33MM) and augments proteasome inhibitor in a murine plasmacytoma model of MM (0.2 mg bortezomib/kg i.v. twice weekly with 30 mg SCIO-469/kg b.i.d. p.o.; RPMI8226). | [in vivo]
Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease[2].
Talmapimod inhibits multiple myeloma growth and prevents bone disease in the 5T2MM and 5T33MM models[3].
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[4]. | Animal Model: | Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors)[4] | | Dosage: | P.o.; twice daily orally for 14 days | | Administration: | 10, 30, 90 mg/kg | | Result: | Dose-dependently reduced tumor growth. |
| [IC 50]
p38α: 9 nM (IC50); p38β: 90 nM (IC50) |
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