SB-505124

SKU: orb1224221

Description

SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6.

Key Properties

• CAS Number: 694433-59-5
• MW: 335.4
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₁N₃O₂
• SMILES: CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1
• Target: ALK
• Solubility: Ethanol: 67 mg/mL (199.76 mM); DMSO: 67 mg/mL (199.76 mM)

Bioactivity

• In Vivo:
  SB-505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but administration of SB-505124 with a single dose of Carboplatin (60 mg/kg) results in durable responses without the need for maintenance therapy in five animals. Animal model: C57Bl6 mice with A549 xenografts. Dosage: 5 mg/kg. Administration: i.p.; daily. Result: Had no effect alone, but administration with a single dose of carboplatin (60 mg/kg) resulted in durable responses without the need for maintenance therapy in five animals.
• In Vitro:
  SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC50 value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells. SB-505124 (10 μM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB505124 | SB-505124 | SB 505124

Quick Database Links

Gene Symbol

ALK