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SB-505124 hydrochloride (SB505124 hydrochloride) is an orally available, selective and potent inhibitor of TGF-β type I receptors (ALK4, ALK5, ALK7) with IC50 values of 129 nM and 47 nM for ALK4 and ALK5, respectively. SB-505124 hydrochloride inhibits IL-6 production by synovial explants and reduces Th17 differentiation in mice by decreasing Il17a and Rorc gene expression and IL-17 protein production.SB-505124 hydrochloride is used in the study of colorectal cancer.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $35 | In Stock | |
5 mg | $73 | In Stock | |
10 mg | $105 | In Stock | |
25 mg | $196 | In Stock | |
50 mg | $328 | In Stock | |
100 mg | $489 | In Stock |
Description | SB-505124 hydrochloride (SB505124 hydrochloride) is an orally available, selective and potent inhibitor of TGF-β type I receptors (ALK4, ALK5, ALK7) with IC50 values of 129 nM and 47 nM for ALK4 and ALK5, respectively. SB-505124 hydrochloride inhibits IL-6 production by synovial explants and reduces Th17 differentiation in mice by decreasing Il17a and Rorc gene expression and IL-17 protein production.SB-505124 hydrochloride is used in the study of colorectal cancer. |
In vitro | METHODS: Rabbit subconjunctival fibroblasts were incubated with 10 μM SB-505124 or 0.04% MMC and then incubated with or without TGF-β2 (2 ng/ml) in 12-well plates for 48 h. The effects of ALK-5 inhibitor SB-505124 on TGF-β2-induced downstream effects were analyzed by Western blotting. RESULTS: The levels of pSmad2, CTGF, and α-SMA in rabbit subconjunctival fibroblasts treated with SB-505124 were decreased in a concentration-dependent manner. [3] |
In vivo | SB-505124 (5 mg/kg; i.p.) alone does not elicit any response in C57Bl6 mice bearing A549 xenografts. However, when combined with a single dose of Carboplatin (60 mg/kg), SB-505124 induces sustained therapeutic effects in five subjects, eliminating the need for ongoing maintenance therapy. This synergy presents a potent treatment strategy without continuous intervention in the specified animal model, highlighting its potential efficacy. |
Alias | SB505124 hydrochloride, SB 505124 hydrochloride |
Molecular Weight | 371.86 |
Formula | C20H22ClN3O2 |
Cas No. | 356559-13-2 |
Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | Methanol: 120 mg/mL (322.70 mM), Sonication is recommended. DMSO: 40 mg/mL (107.57 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/Methanol
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