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Talmapimod (SCIO-469) is a selective, orally active, ATP-competitive p38α inhibitor with IC50 values of 9 nM for p38α and 90 nM for p38β. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $48 | In Stock | |
2 mg | $70 | In Stock | |
5 mg | $117 | In Stock | |
10 mg | $187 | In Stock | |
25 mg | $397 | In Stock | |
50 mg | $589 | In Stock | |
100 mg | $843 | In Stock | |
1 mL x 10 mM (in DMSO) | $133 | In Stock |
Description | Talmapimod (SCIO-469) is a selective, orally active, ATP-competitive p38α inhibitor with IC50 values of 9 nM for p38α and 90 nM for p38β. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs. |
Targets&IC50 | p38β:90 nM, p38α:9 nM |
In vitro | phosphorylation of p38 MAPK inhibited by Talmapimod (100-200 nM; 1 hour) in MM cells[1].In human whole blood, LPS-induced TNF-a production inhibited by Talmapimod [2]. Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells[3]. |
In vivo | Talmapimod (SCIO-469), targeting p38α MAPK, reduces myeloma burden and prevents myeloma bone disease[2]. In 5T2MM and 5T33MM models, it inhibits multiple myeloma growth and bone diseases[3]. Administered at 10-90 mg/kg orally, twice daily for 14 days, Talmapimod dose-dependently diminishes tumor growth and decreases the weight of palpable tumors at termination[4]. |
Alias | SCIO-469 |
Molecular Weight | 513 |
Formula | C27H30ClFN4O3 |
Cas No. | 309913-83-5 |
Smiles | C[C@H]1CN([C@H](C)CN1Cc1ccc(F)cc1)C(=O)c1cc2c(cn(C)c2cc1Cl)C(=O)C(=O)N(C)C |
Relative Density. | 1.29 g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 95 mg/mL (185.19 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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