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MedKoo Cat#: 125956 | Name: Halofuginone lactate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

Chemical Structure

Halofuginone lactate
Halofuginone lactate
CAS#82186-71-8 (lactate)

Theoretical Analysis

MedKoo Cat#: 125956

Name: Halofuginone lactate

CAS#: 82186-71-8 (lactate)

Chemical Formula: C19H23BrClN3O6

Exact Mass: 0.0000

Molecular Weight: 504.76

Elemental Analysis: C, 45.21; H, 4.59; Br, 15.83; Cl, 7.02; N, 8.32; O, 19.02

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 950.00 2 Weeks
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Related CAS #
55837-20-2 (free base) 64924-67-0 (HBr) 1217623-74-9 (HCl) 82186-71-8 (lactate)
Synonym
Halofuginone lactate; Halagon; RU 19110; RU19110; RU-19110; Halofuginone; Tempostatin
IUPAC/Chemical Name
7-bromo-6-chloro-3-(3-((2S,3R)-3-hydroxypiperidin-2-yl)-2-oxopropyl)quinazolin-4(3H)-one, 2-hydroxypropanoic acid
InChi Key
GATQERNJKZPJNX-LDXVYITESA-N
InChi Code
InChI=1S/C16H17BrClN3O3.C3H6O3/c17-11-6-13-10(5-12(11)18)16(24)21(8-20-13)7-9(22)4-14-15(23)2-1-3-19-14;1-2(4)3(5)6/h5-6,8,14-15,19,23H,1-4,7H2;2,4H,1H3,(H,5,6)/t14-,15+;/m0./s1
SMILES Code
O=C1N(C=NC2=C1C=C(C(Br)=C2)Cl)CC(C[C@@H]3NCCC[C@H]3O)=O.OC(C(C)O)=O
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 504.76 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.

Recalculate based on batch purity %
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
1: Pines M, Spector I. Halofuginone - The Multifaceted Molecule. Molecules. 2015 Jan 5;20(1):573-594. Review. PubMed PMID: 25569515. 2: Pines M. Halofuginone for fibrosis, regeneration and cancer in the gastrointestinal tract. World J Gastroenterol. 2014 Oct 28;20(40):14778-86. doi: 10.3748/wjg.v20.i40.14778. PubMed PMID: 25356039; PubMed Central PMCID: PMC4209542. 3: Guo LW, Wang B, Goel SA, Little C, Takayama T, Shi XD, Roenneburg D, DiRenzo D, Kent KC. Halofuginone stimulates adaptive remodeling and preserves re-endothelialization in balloon-injured rat carotid arteries. Circ Cardiovasc Interv. 2014 Aug;7(4):594-601. doi: 10.1161/CIRCINTERVENTIONS.113.001181. Epub 2014 Jul 29. PubMed PMID: 25074254; PubMed Central PMCID: PMC4140988. 4: Park MK, Park JS, Park EM, Lim MA, Kim SM, Lee DG, Baek SY, Yang EJ, Woo JW, Lee J, Kwok SK, Kim HY, Cho ML, Park SH. Halofuginone ameliorates autoimmune arthritis in mice by regulating the balance between Th17 and Treg cells and inhibiting osteoclastogenesis. Arthritis Rheumatol. 2014 May;66(5):1195-207. doi: 10.1002/art.38313. PubMed PMID: 24782183. 5: Bodanovsky A, Guttman N, Barzilai-Tutsch H, Genin O, Levy O, Pines M, Halevy O. Halofuginone improves muscle-cell survival in muscular dystrophies. Biochim Biophys Acta. 2014 Jul;1843(7):1339-47. doi: 10.1016/j.bbamcr.2014.03.025. Epub 2014 Apr 2. PubMed PMID: 24703880. 6: McLaughlin NP, Evans P, Pines M. The chemistry and biology of febrifugine and halofuginone. Bioorg Med Chem. 2014 Apr 1;22(7):1993-2004. doi: 10.1016/j.bmc.2014.02.040. Epub 2014 Mar 1. Review. PubMed PMID: 24650700. 7: Petermann J, Paraud C, Pors I, Chartier C. Efficacy of halofuginone lactate against experimental cryptosporidiosis in goat neonates. Vet Parasitol. 2014 May 28;202(3-4):326-9. doi: 10.1016/j.vetpar.2014.02.027. Epub 2014 Feb 22. PubMed PMID: 24636788. 8: Kapoor S. Reduction of burn scar formation by halofuginone-eluting silicone gel sheets: a controlled study on nude mice. Ann Plast Surg. 2014 Apr;72(4):489. doi: 10.1097/SAP.0b013e318281ad59. PubMed PMID: 24618743. 9: Carlson TJ, Pellerin A, Djuretic IM, Trivigno C, Koralov SB, Rao A, Sundrud MS. Halofuginone-induced amino acid starvation regulates Stat3-dependent Th17 effector function and reduces established autoimmune inflammation. J Immunol. 2014 Mar 1;192(5):2167-76. doi: 10.4049/jimmunol.1302316. Epub 2014 Jan 31. PubMed PMID: 24489094; PubMed Central PMCID: PMC3936195. 10: Jin C, Jia Y, Jin C, Dong H, Cheng P, Zhou J, Wang Y, Zheng B, Liu F. Therapeutic effect of Halofuginone on ITP mice by regulating the differentiation of Th cell subsets. Int Immunopharmacol. 2014 Feb;18(2):213-6. doi: 10.1016/j.intimp.2013.12.013. Epub 2013 Dec 22. PubMed PMID: 24368123. 11: Liang J, Zhang B, Shen RW, Liu JB, Gao MH, Li Y, Li YY, Zhang W. Preventive effect of halofuginone on concanavalin A-induced liver fibrosis. PLoS One. 2013 Dec 16;8(12):e82232. doi: 10.1371/journal.pone.0082232. eCollection 2013. PubMed PMID: 24358159; PubMed Central PMCID: PMC3864948. 12: Jin ML, Park SY, Kim YH, Park G, Lee SJ. Halofuginone induces the apoptosis of breast cancer cells and inhibits migration via downregulation of matrix metalloproteinase-9. Int J Oncol. 2014 Jan;44(1):309-18. doi: 10.3892/ijo.2013.2157. Epub 2013 Oct 31. PubMed PMID: 24173318. 13: Son J, Lee EH, Park M, Kim JH, Kim J, Kim S, Jeon YH, Hwang KY. Conformational changes in human prolyl-tRNA synthetase upon binding of the substrates proline and ATP and the inhibitor halofuginone. Acta Crystallogr D Biol Crystallogr. 2013 Oct;69(Pt 10):2136-45. doi: 10.1107/S0907444913020556. Epub 2013 Sep 20. PubMed PMID: 24100331. 14: Zeplin PH. Halofuginone down-regulates Smad3 expression and inhibits the TGFbeta-induced expression of fibrotic markers in human corneal fibroblasts. Ann Plast Surg. 2014 Apr;72(4):489. doi: 10.1097/SAP.0b013e31828a49e3. PubMed PMID: 23845969. 15: Almawly J, Prattley D, French NP, Lopez-Villalobos N, Hedgespeth B, Grinberg A. Utility of halofuginone lactate for the prevention of natural cryptosporidiosis of calves, in the presence of co-infection with rotavirus and Salmonella Typhimurium. Vet Parasitol. 2013 Oct 18;197(1-2):59-67. doi: 10.1016/j.vetpar.2013.04.029. Epub 2013 Apr 24. PubMed PMID: 23707392. 16: Chu TL, Guan Q, Nguan CY, Du C. Halofuginone suppresses T cell proliferation by blocking proline uptake and inducing cell apoptosis. Int Immunopharmacol. 2013 Aug;16(4):414-23. doi: 10.1016/j.intimp.2013.04.031. Epub 2013 May 16. PubMed PMID: 23685128. 17: Keidel J, Daugschies A. Integration of halofuginone lactate treatment and disinfection with p-chloro-m-cresol to control natural cryptosporidiosis in calves. Vet Parasitol. 2013 Sep 23;196(3-4):321-6. doi: 10.1016/j.vetpar.2013.03.003. Epub 2013 Mar 14. PubMed PMID: 23561324. 18: Yavas G, Calik M, Calik G, Yavas C, Ata O, Esme H. The effect of Halofuginone in the amelioration of radiation induced-lung fibrosis. Med Hypotheses. 2013 Apr;80(4):357-9. doi: 10.1016/j.mehy.2013.01.001. Epub 2013 Jan 23. PubMed PMID: 23352286. 19: Halevy O, Genin O, Barzilai-Tutsch H, Pima Y, Levi O, Moshe I, Pines M. Inhibition of muscle fibrosis and improvement of muscle histopathology in dysferlin knock-out mice treated with halofuginone. Histol Histopathol. 2013 Feb;28(2):211-26. PubMed PMID: 23275304. 20: Juárez P, Mohammad KS, Yin JJ, Fournier PG, McKenna RC, Davis HW, Peng XH, Niewolna M, Javelaud D, Chirgwin JM, Mauviel A, Guise TA. Halofuginone inhibits the establishment and progression of melanoma bone metastases. Cancer Res. 2012 Dec 1;72(23):6247-56. doi: 10.1158/0008-5472.CAN-12-1444. Epub 2012 Sep 20. PubMed PMID: 23002206.