Name: Halofuginone hydrobromide | RU-19110 hydrobromide; Halofuginone(hydrobromide)
Brand: Ambeed
SKU: A446753
Rating: 4.5 (122 reviews)

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CAS No. :	64924-67-0
Formula :	C₁₆H₁₈Br₂ClN₃O₃
M.W :	495.59
SMILES Code :	O=C1N(CC(C[C@H]2NCCC[C@@H]2O)=O)C=NC3=C1C=C(Cl)C(Br)=C3.[H]Br
Synonyms :	RU-19110 hydrobromide; Halofuginone(hydrobromide)
MDL No. :	MFCD00946455

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H302-H315-H319-H335
Precautionary Statements:	P261-P305+P351+P338

Human hepatoma cells (HepG2)	50 nM	6 hours	To study the effect of HF on GCN2 and ISR, results showed HF increased levels of P-eIF2α and P-GCN2, and induced ATF4 protein expression.	Nucleic Acids Res. 2021 Jun 4;49(10):5726-5742
Mouse embryonic fibroblast (MEF) cells	100 nM	6 hours	To study the effect of HF on GCN2 and ISR, results showed HF increased levels of P-eIF2α and P-GCN2, and induced ATF4 protein expression.	Nucleic Acids Res. 2021 Jun 4;49(10):5726-5742
NIH/3T3 mouse fibroblasts	100 nM		Identified EPRS-regulated proline-rich genes via RNA-Seq and polysome profiling-Seq	Circ Res. 2020 Aug 28;127(6):827-846
primary cardiac fibroblasts	100 nM		Halofuginone significantly decreases translation efficiency of proline-rich collagens	Circ Res. 2020 Aug 28;127(6):827-846
human primary pancreatic stellate cells	50 nM and 100 nM	48 hours	inhibited α-SMA expression, reduced fibrosis-related genes (e.g., type-I collagen and hyaluronan synthase 2), and decreased cell proliferation	Cancer Res. 2019 Jan 15;79(2):372-386
murine primary pancreatic stellate cells	50 nM and 100 nM	48 hours	inhibited α-SMA expression, reduced fibrosis-related genes (e.g., type-I collagen and hyaluronan synthase 2), and decreased cell proliferation	Cancer Res. 2019 Jan 15;79(2):372-386
mouse primary hepatocytes	25 nM	24 hours	To investigate the effect of Halofuginone on the expression of ATF4, GDF15, and FGF21 genes, results showed that HF upregulated the expression of these genes.	Sci Adv. 2025 Mar 28;11(13):eadt3142
CD8+ T cells	50 ng/mL	48 hours	Enhanced effector function and oxidative metabolism, increased production of IFN-γ, TNF-α, and IL-2, as well as granzyme B expression.	Cell Rep Med. 2024 Mar 19;5(3):101465
HUVEC cells	50, 100, 200 ng/mL	24 hours	HF increased VEGF gene expression and protein secretion but had no significant effect on the gene expression of ANGPT-1, HIF-1α, TIMP2, and CXCL10.	J Exp Clin Cancer Res. 2015 Jun 23;34(1):65
NB4 cells	50, 100, 200 ng/mL	6, 12, 24, 72 hours	HF downregulated the expression of proangiogenic factors, upregulated the antiangiogenic factors TIMP2 and CXCL10, and reduced VEGF secretion and SMAD2 phosphorylation.	J Exp Clin Cancer Res. 2015 Jun 23;34(1):65
293T cells	50 nM	24 hours	Halofuginone treatment significantly decreased the expression of NRF2-Δ100aa and NRF2-C but had no obvious effect on NRF2-N expression.	Redox Biol. 2022 Feb;49:102224
K4 fibroblast-like synoviocytes	250 nM	24 hours	Suppressed TNF-α-induced inflammatory gene expression, persisting in GCN2-depleted cells	Proc Natl Acad Sci U S A. 2020 Apr 21;117(16):8900-8911
lung fibroblasts	200 nM	6 hours	Inhibited TGF-β-induced smooth muscle actin and CTGF expression	Proc Natl Acad Sci U S A. 2020 Apr 21;117(16):8900-8911
human umbilical vein endothelial cells (HUVEC)	200 nM	16 hours	Inhibited TNF-α or IL-1β-induced VCAM-1 and E-selectin expression	Proc Natl Acad Sci U S A. 2020 Apr 21;117(16):8900-8911
rheumatoid arthritis fibroblast-like synoviocytes (RA-FLS)	200 nM	16 hours	Inhibited TNF-α or IL-1β-induced MMP13 expression, reversible by excess proline	Proc Natl Acad Sci U S A. 2020 Apr 21;117(16):8900-8911
mouse embryonic fibroblasts (MEFs)	12.5 nM or 200 nM	5h	HF-induced eIF2α phosphorylation is entirely dependent on GCN2	EMBO J. 2022 Jun 1;41(11):e109985
HeLa cells	12.5 nM to 312.5 nM	5h	Induced ISR response, manifested by increased phosphorylation of eIF2α and elevated levels of ATF4, R15A	EMBO J. 2022 Jun 1;41(11):e109985
Human CD8+ T cells	12.5 ng/mL	5 days	Enhanced oxidative metabolism and effector function, increased expression of 4-1BB and CD98.	Cell Rep Med. 2024 Mar 19;5(3):101465
HepG2 cells	0-200 nM	24 hours	Halofuginone treatment decreased the expression of NRF2, HO-1, and NQO-1, and this reduction was achieved through the proteasome pathway.	Redox Biol. 2022 Feb;49:102224

Mice	Wild-type and Gcn2 knockout mice	Intraperitoneal injection	0.5 mg/kg	Once daily for 1 or 2 days	To study the effect of HF on ISR and mTORC1 signaling in liver, results showed HF activated GCN2-mediated ISR and mTORC1 signaling, with Gcn2 knockout mice showing greater mTORC1 activation and liver steatosis.	Nucleic Acids Res. 2021 Jun 4;49(10):5726-5742
C57BL/6J mice and Lewis rats	Anterior cruciate ligament transection (ACLT) model	Intraperitoneal injection	1 mg/kg body weight	Injected every other day for 1 month	HF attenuated OA progression by inhibiting Th17-induced osteoclastogenesis, TGF-β-dependent Smad2/3 phosphorylation, and angiogenesis.	Ann Rheum Dis. 2016 Sep;75(9):1714-21
Mice	Diet-induced obese (DIO) mice model	Intraperitoneal injection	100 μg/kg	Every 2 days for 8 weeks	To evaluate the effects of Halofuginone on body weight, fat mass, energy expenditure, and food intake in obese mice, results showed that HF significantly reduced body weight and fat mass, increased energy expenditure, and suppressed food intake.	Sci Adv. 2025 Mar 28;11(13):eadt3142
NOD/SCID mice	Acute Promyelocytic Leukemia transplanted model	Intraperitoneal injection	150 μg/kg/day	Once daily for 21 days	HF treatment significantly reduced leukemia burden, decreased the number of VEGF-positive cells, and reduced the gene expression of VEGF, HIF-1α, and ANGPT-2.	J Exp Clin Cancer Res. 2015 Jun 23;34(1):65
C57BL/6 mice	Regular chow-fed mice	Intraperitoneal injection	3 mg/kg	3 days	Halofuginone treatment decreased the protein expression of NRF2, HO-1, and NQO-1 in the liver.	Redox Biol. 2022 Feb;49:102224
Mice	GCN2 knockout mice	In vitro culture	10 nM	4-day polarization culture	HF inhibited TH17 differentiation and IL-23-induced IL-17A production in memory TH17 cells independent of GCN2 signaling	Proc Natl Acad Sci U S A. 2020 Apr 21;117(16):8900-8911
Rats	TNBS-induced chronic pancreatitis model	Intraperitoneal injection	200 μg/kg	14 days	Halofuginone significantly reduced phosphorylated SMAD3 expression in the DRG and attenuated pancreatic hyperalgesia in CP rats	Gastroenterology. 2018 Jun;154(8):2252-2265. e2
Mice	KPC genetically engineered mouse model	Intraperitoneal injection	0.75 mg/kg	3 times/week, total of 5 doses	HF treatment reduced PSC activation and ECM production, decreased tumor interstitial pressure, improved drug distribution, promoted anti-tumor immune cell infiltration, and resulted in tumor necrosis and volume reduction	Cancer Res. 2019 Jan 15;79(2):372-386

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NCT00027677	Unspecified Adult Solid Tumor,... More >> Protocol Specific Less <<	Phase 1	Completed	-	Belgium ... More >> U.Z. Gasthuisberg Leuven, Belgium, B-3000 Netherlands University Hospital - Rotterdam Dijkzigt Rotterdam, Netherlands, 3000 CA Daniel Den Hoed Cancer Center at Erasmus Medical Center Rotterdam, Netherlands, 3008 AE Less <<
NCT02525302	Duchenne Muscular Dystrophy	Phase 2	Terminated(Dosing stopped)	-	United States, California ... More >> University of California, Davis Medical Center Sacramento, California, United States, 95817 United States, Maryland Kennedy Krieger Institute, Johns Hopkins School of Medicine Baltimore, Maryland, United States, 21205 United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States, 63110 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229 Nationwide Children's Hospital Columbus, Ohio, United States, 43205 Less <<
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Bio Calculators
Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	2.02mL 0.40mL 0.20mL	10.09mL 2.02mL 1.01mL	20.18mL 4.04mL 2.02mL
Dissolving Methods	Animal experiment Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn: in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound. Protocol 1 Protocol 2

Precautionary Statements-General
Code	Phrase
P101	If medical advice is needed,have product container or label at hand.
P102	Keep out of reach of children.
P103	Read label before use
Prevention
Code	Phrase
P201	Obtain special instructions before use.
P202	Do not handle until all safety precautions have been read and understood.
P210	Keep away from heat/sparks/open flames/hot surfaces. - No smoking.
P211	Do not spray on an open flame or other ignition source.
P220	Keep/Store away from clothing/combustible materials.
P221	Take any precaution to avoid mixing with combustibles
P222	Do not allow contact with air.
P223	Keep away from any possible contact with water, because of violent reaction and possible flash fire.
P230	Keep wetted
P231	Handle under inert gas.
P232	Protect from moisture.
P233	Keep container tightly closed.
P234	Keep only in original container.
P235	Keep cool
P240	Ground/bond container and receiving equipment.
P241	Use explosion-proof electrical/ventilating/lighting/equipment.
P242	Use only non-sparking tools.
P243	Take precautionary measures against static discharge.
P244	Keep reduction valves free from grease and oil.
P250	Do not subject to grinding/shock/friction.
P251	Pressurized container: Do not pierce or burn, even after use.
P260	Do not breathe dust/fume/gas/mist/vapours/spray.
P261	Avoid breathing dust/fume/gas/mist/vapours/spray.
P262	Do not get in eyes, on skin, or on clothing.
P263	Avoid contact during pregnancy/while nursing.
P264	Wash hands thoroughly after handling.
P265	Wash skin thouroughly after handling.
P270	Do not eat, drink or smoke when using this product.
P271	Use only outdoors or in a well-ventilated area.
P272	Contaminated work clothing should not be allowed out of the workplace.
P273	Avoid release to the environment.
P280	Wear protective gloves/protective clothing/eye protection/face protection.
P281	Use personal protective equipment as required.
P282	Wear cold insulating gloves/face shield/eye protection.
P283	Wear fire/flame resistant/retardant clothing.
P284	Wear respiratory protection.
P285	In case of inadequate ventilation wear respiratory protection.
P231 + P232	Handle under inert gas. Protect from moisture.
P235 + P410	Keep cool. Protect from sunlight.
Response
Code	Phrase
P301	IF SWALLOWED:
P304	IF INHALED:
P305	IF IN EYES:
P306	IF ON CLOTHING:
P307	IF exposed:
P308	IF exposed or concerned:
P309	IF exposed or if you feel unwell:
P310	Immediately call a POISON CENTER or doctor/physician.
P311	Call a POISON CENTER or doctor/physician.
P312	Call a POISON CENTER or doctor/physician if you feel unwell.
P313	Get medical advice/attention.
P314	Get medical advice/attention if you feel unwell.
P315	Get immediate medical advice/attention.
P320
P302 + P352	IF ON SKIN: wash with plenty of soap and water.
P321
P322
P330	Rinse mouth.
P331	Do NOT induce vomiting.
P332	IF SKIN irritation occurs:
P333	If skin irritation or rash occurs:
P334	Immerse in cool water/wrap n wet bandages.
P335	Brush off loose particles from skin.
P336	Thaw frosted parts with lukewarm water. Do not rub affected area.
P337	If eye irritation persists:
P338	Remove contact lenses, if present and easy to do. Continue rinsing.
P340	Remove victim to fresh air and keep at rest in a position comfortable for breathing.
P341	If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P342	If experiencing respiratory symptoms:
P350	Gently wash with plenty of soap and water.
P351	Rinse cautiously with water for several minutes.
P352	Wash with plenty of soap and water.
P353	Rinse skin with water/shower.
P360	Rinse immediately contaminated clothing and skin with plenty of water before removing clothes.
P361	Remove/Take off immediately all contaminated clothing.
P362	Take off contaminated clothing and wash before reuse.
P363	Wash contaminated clothing before reuse.
P370	In case of fire:
P371	In case of major fire and large quantities:
P372	Explosion risk in case of fire.
P373	DO NOT fight fire when fire reaches explosives.
P374	Fight fire with normal precautions from a reasonable distance.
P376	Stop leak if safe to do so. Oxidising gases (section 2.4) 1
P377	Leaking gas fire: Do not extinguish, unless leak can be stopped safely.
P378
P380	Evacuate area.
P381	Eliminate all ignition sources if safe to do so.
P390	Absorb spillage to prevent material damage.
P391	Collect spillage. Hazardous to the aquatic environment
P301 + P310	IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P301 + P312	IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P301 + P330 + P331	IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.
P302 + P334	IF ON SKIN: Immerse in cool water/wrap in wet bandages.
P302 + P350	IF ON SKIN: Gently wash with plenty of soap and water.
P303 + P361 + P353	IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.
P304 + P312	IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell.
P304 + P340	IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P304 + P341	IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P305 + P351 + P338	IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.
P306 + P360	IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes.
P307 + P311	IF exposed: call a POISON CENTER or doctor/physician.
P308 + P313	IF exposed or concerned: Get medical advice/attention.
P309 + P311	IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician.
P332 + P313	IF SKIN irritation occurs: Get medical advice/attention.
P333 + P313	IF SKIN irritation or rash occurs: Get medical advice/attention.
P335 + P334	Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages.
P337 + P313	IF eye irritation persists: Get medical advice/attention.
P342 + P311	IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician.
P370 + P376	In case of fire: Stop leak if safe to Do so.
P370 + P378	In case of fire:
P370 + P380	In case of fire: Evacuate area.
P370 + P380 + P375	In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion.
P371 + P380 + P375	In case of major fire and large quantities: Evacuate area. Fight fire remotely due to the risk of explosion.
Storage
Code	Phrase
P401
P402	Store in a dry place.
P403	Store in a well-ventilated place.
P404	Store in a closed container.
P405	Store locked up.
P406	Store in corrosive resistant/ container with a resistant inner liner.
P407	Maintain air gap between stacks/pallets.
P410	Protect from sunlight.
P411
P412	Do not expose to temperatures exceeding 50 oC/ 122 oF.
P413
P420	Store away from other materials.
P422
P402 + P404	Store in a dry place. Store in a closed container.
P403 + P233	Store in a well-ventilated place. Keep container tightly closed.
P403 + P235	Store in a well-ventilated place. Keep cool.
P410 + P403	Protect from sunlight. Store in a well-ventilated place.
P410 + P412	Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF.
P411 + P235	Keep cool.
Disposal
Code	Phrase
P501	Dispose of contents/container to ...
P502	Refer to manufacturer/supplier for information on recovery/recycling

Physical hazards
Code	Phrase
H200	Unstable explosive
H201	Explosive; mass explosion hazard
H202	Explosive; severe projection hazard
H203	Explosive; fire, blast or projection hazard
H204	Fire or projection hazard
H205	May mass explode in fire
H220	Extremely flammable gas
H221	Flammable gas
H222	Extremely flammable aerosol
H223	Flammable aerosol
H224	Extremely flammable liquid and vapour
H225	Highly flammable liquid and vapour
H226	Flammable liquid and vapour
H227	Combustible liquid
H228	Flammable solid
H229	Pressurized container: may burst if heated
H230	May react explosively even in the absence of air
H231	May react explosively even in the absence of air at elevated pressure and/or temperature
H240	Heating may cause an explosion
H241	Heating may cause a fire or explosion
H242	Heating may cause a fire
H250	Catches fire spontaneously if exposed to air
H251	Self-heating; may catch fire
H252	Self-heating in large quantities; may catch fire
H260	In contact with water releases flammable gases which may ignite spontaneously
H261	In contact with water releases flammable gas
H270	May cause or intensify fire; oxidizer
H271	May cause fire or explosion; strong oxidizer
H272	May intensify fire; oxidizer
H280	Contains gas under pressure; may explode if heated
H281	Contains refrigerated gas; may cause cryogenic burns or injury
H290	May be corrosive to metals
Health hazards
Code	Phrase
H300	Fatal if swallowed
H301	Toxic if swallowed
H302	Harmful if swallowed
H303	May be harmful if swallowed
H304	May be fatal if swallowed and enters airways
H305	May be harmful if swallowed and enters airways
H310	Fatal in contact with skin
H311	Toxic in contact with skin
H312	Harmful in contact with skin
H313	May be harmful in contact with skin
H314	Causes severe skin burns and eye damage
H315	Causes skin irritation
H316	Causes mild skin irritation
H317	May cause an allergic skin reaction
H318	Causes serious eye damage
H319	Causes serious eye irritation
H320	Causes eye irritation
H330	Fatal if inhaled
H331	Toxic if inhaled
H332	Harmful if inhaled
H333	May be harmful if inhaled
H334	May cause allergy or asthma symptoms or breathing difficulties if inhaled
H335	May cause respiratory irritation
H336	May cause drowsiness or dizziness
H340	May cause genetic defects
H341	Suspected of causing genetic defects
H350	May cause cancer
H351	Suspected of causing cancer
H360	May damage fertility or the unborn child
H361	Suspected of damaging fertility or the unborn child
H361d	Suspected of damaging the unborn child
H362	May cause harm to breast-fed children
H370	Causes damage to organs
H371	May cause damage to organs
H372	Causes damage to organs through prolonged or repeated exposure
H373	May cause damage to organs through prolonged or repeated exposure
Environmental hazards
Code	Phrase
H400	Very toxic to aquatic life
H401	Toxic to aquatic life
H402	Harmful to aquatic life
H410	Very toxic to aquatic life with long-lasting effects
H411	Toxic to aquatic life with long-lasting effects
H412	Harmful to aquatic life with long-lasting effects
H413	May cause long-lasting harmful effects to aquatic life
H420	Harms public health and the environment by destroying ozone in the upper atmosphere

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CAS No.: 64924-67-0

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CAS No.: 64924-67-0

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