Talmapimod hydrochloride structure
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Common Name | Talmapimod hydrochloride | ||
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CAS Number | 309915-12-6 | Molecular Weight | 549.46 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C27H31Cl2FN4O3 | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of Talmapimod hydrochlorideTalmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs[1][2][3]. |
Name | Talmapimod hydrochloride |
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Description | Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs[1][2][3]. |
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Related Catalog | |
Target |
p38α:9 nM (IC50) p38β:90 nM (IC50) |
In Vitro | Talmapimod (SCIO-469) hydrochloride (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells[1]. Talmapimod hydrochloride inhibits LPS-induced TNF-a production in human whole blood[2]. Talmapimod hydrochloride decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells[3]. Western Blot Analysis[1] 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. |
In Vivo | Talmapimod hydrochloride (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: 10, 30, 90 mg/kg Administration: P.o.; twice daily orally for 14 days Result: Dose-dependently reduced tumor growth. |
References |
Molecular Formula | C27H31Cl2FN4O3 |
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Molecular Weight | 549.46 |