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Halofuginone hydrobromide

Cat. No. 1993 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: High affinity competitive prolyl-tRNA synthetase inhibitor
Chemical Name: (2R*,3S*)-7-Bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4-3H-quinazolinone hydrobromide
Purity: ≥98% (HPLC)
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for Halofuginone hydrobromide

Halofuginone hydrobromide is a high affinity competitive prolyl-tRNA synthetase inhibitor (Ki = 18.3 nM). Blocks expression of MMP2. Inhibits ECM invasion in vitro and lung metastasis by bladder cancer cells in mice. Inhibits the development of Th17-driven autoimmunity in a mouse model of multiple sclerosis by activating the amino acid response (AAR) pathway. Also antiparasitic.

Technical Data for Halofuginone hydrobromide

M. Wt 495.59
Formula C16H17BrClN3O3.HBr
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 64924-67-0
PubChem ID 400771
InChI Key SJUWEPZBTXEUMU-LDXVYITESA-N
Smiles BrC1=CC2=C(C(N(CC(C[C@@H]3[C@H](O)CCCN3)=O)C=N2)=O)C=C1Cl.Br

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Halofuginone hydrobromide

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 49.56 100

Preparing Stock Solutions for Halofuginone hydrobromide

The following data is based on the product molecular weight 495.59. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.02 mL 10.09 mL 20.18 mL
5 mM 0.4 mL 2.02 mL 4.04 mL
10 mM 0.2 mL 1.01 mL 2.02 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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Product Datasheets for Halofuginone hydrobromide

Certificate of Analysis / Product Datasheet
Safety Datasheet

References for Halofuginone hydrobromide

References are publications that support the biological activity of the product.

Anderson et al (1979) Analysis of the anti-coccidial drug, halofunginone, in chicken feed using gas-liquid chromatography and high-performance liquid chromatography. J.Chromatogr. 168 471 PMID: 570196

Elkin et al (1999) Inhibition of matrix metalloproteinase-2 expression and bladder carcinoma metastasis by halofuginone. Clin.Cancer.Res. 5 1982 PMID: 10473075

Keller et al (2012) Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 8 311 PMID: 22327401

If you know of a relevant reference for Halofuginone hydrobromide, please let us know.

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Citations for Halofuginone hydrobromide

Citations are publications that use Tocris products.

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