Halofuginone (RU-19110) is a synthetic derivative of febrifugine with potent antifibrotic, antiproliferative, antiangiogenic, and immunomodulatory activities. It exerts its primary bioactivity by inhibiting prolyl-tRNA synthetase, leading to activation of the amino acid starvation response and inhibition of collagen type I synthesis. In fibroblasts, halofuginone reduces TGF-β–induced collagen α1(I) mRNA expression with an IC₅₀ in the low nanomolar range (typically ~10 nM). In preclinical cancer models, halofuginone inhibits tumor growth and metastasis, partly via antiangiogenic mechanisms, with effective concentrations ranging from 10 to 100 nM in vitro. Additionally, it has been shown to suppress Th17 cell differentiation by blocking TGF-β signaling, demonstrating immunoregulatory potential in autoimmune disease models
MedKoo Cat#: 563947
Name: Halofuginone HBr
CAS#: 64924-67-0 (HBr)
Chemical Formula: C16H18Br2ClN3O3
Exact Mass: 0.0000
Molecular Weight: 495.60
Elemental Analysis: C, 38.78; H, 3.66; Br, 32.25; Cl, 7.15; N, 8.48; O, 9.68
The following data is based on the product molecular weight 495.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
