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CAS No. :	1345407-05-7
Formula :	C₇₈H₁₀₆N₁₈O₉
M.W :	1439.79
SMILES Code :	O=C(N[C@@H](CCCCN)C(N[C@@H](CC1=CNC2=C1C=CC=C2)C(N[C@@H](CC3=CNC4=C3C=CC=C4)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CC5=CNC6=C5C=CC=C6)C(N[C@@H](C(C7=CC=CC=C7)C8=CC=CC=C8)C(N[C@H](C(N)=O)CCCCN)=O)=O)=O)=O)=O)=O)=O)[C@@H](N)CCCCN
Synonyms :	LTX 315
MDL No. :	MFCD30742993
InChI Key :	GGAKLYWEFZCVIT-TVEKFXMRSA-N
Pubchem ID :	46200994

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

U2OS osteosarcoma cells	100 mg/ml	6 hours	Observed necrotic morphology in cells	Cell Cycle. 2015;14(21):3506-12
B16F1 (murine melanoma cells)	35 µM (IC100)	15 minutes	Evaluate the kill kinetics of LTX-315 on B16F1 cells, showing cell lysis within 15 minutes.	Cancer Immunol Immunother. 2014 Jun;63(6):601-13
Rat transformed mesenchymal stem cells (rTMSC)	7 µM (IC50)	2 hours	To evaluate the cytotoxic effect of LTX-315, results showed that LTX-315 exhibited faster cytotoxic effects compared to conventional chemotherapeutic drugs within 2 hours.	Oncoimmunology. 2017 Jun 16;6(8):e1338236
A375 (human melanoma cells)	11 µM (IC50)	2 hours	Evaluate the cytotoxic effect of LTX-315 on A375 cells, showing rapid cytotoxicity within 2 hours.	Cancer Immunol Immunother. 2014 Jun;63(6):601-13
B16F1 (murine melanoma cells)	13 µM (IC50)	2 hours	Evaluate the cytotoxic effect of LTX-315 on B16F1 cells, showing rapid cytotoxicity within 2 hours.	Cancer Immunol Immunother. 2014 Jun;63(6):601-13
Luc/RFP-positive McA-RH7777 cells	40.98 µg/mL (IC50)	24 hours	To evaluate the anti-proliferative effects of LTX-315 and liposomal doxorubicin on HCC cells. Results showed that both LTX-315 and liposomal doxorubicin exhibited dose-dependent anti-proliferative effects.	J Immunother Cancer. 2022 Nov;10(11):e005619
B16-F10	104.3 ± 28.5 µM (IC50)	24 hours	Evaluate the antiproliferative activity of LTX-315 on B16-F10 cells	Acta Pharmacol Sin. 2023 Jan;44(1):201-210
HepG2	109.8 ± 16.0 µM (IC50)	24 hours	Evaluate the antiproliferative activity of LTX-315 on HepG2 cells	Acta Pharmacol Sin. 2023 Jan;44(1):201-210
HeLa	127.8 ± 13.4 µM (IC50)	24 hours	Evaluate the antiproliferative activity of LTX-315 on HeLa cells	Acta Pharmacol Sin. 2023 Jan;44(1):201-210
VX2 tumor cells	27.65 µM (IC50)	30 minutes	To validate the killing effect of RFH-enhanced LTX-315 on VX2 tumor cells. Results showed that the combination therapy group had the lowest cell viability and the highest apoptosis rate compared to RFH or LTX-315 alone.	Cancers (Basel). 2022 Dec 11;14(24):6093
4T1 cells	10 μg/ml	48 hours	To evaluate the inhibitory effect of LTX/siR-NPs on TGF-β1 expression and their ability to induce immunogenic cell death (ICD). Results showed that LTX/siR-NPs significantly inhibited TGF-β1 expression and induced ICD, as evidenced by increased levels of danger molecules (e.g., calreticulin, ATP, and HMGB1).	Bioeng Transl Med. 2022 Aug 11;8(5):e10392
Mouse bone marrow-derived dendritic cells (muDCs)	20 ng/ml	48 hours	LTX-315 upregulated the expression of CD80, CD86, and I-A/E, as well as the production of IL-1β, indicating that LTX-315 can directly induce mouse DC maturation.	Front Immunol. 2024 Mar 13;15:1332922
Human monocyte-derived dendritic cells (monoDCs)	20 ng/ml	48 hours	LTX-315 upregulated the expression of co-stimulatory molecules (CD80, CD83, and CD86) and HLA-DR, as well as the production of TNFα, indicating that LTX-315 possesses the capacity to directly induce DC maturation.	Front Immunol. 2024 Mar 13;15:1332922
Rat transformed mesenchymal stem cells (rTMSC)	17 µM (IC50)	5, 10, 30, 60 minutes	To study whether LTX-315 could induce the release of DAMPs, results showed that LTX-315-treated cells rapidly released ATP, cytochrome c, and HMGB1.	Oncoimmunology. 2017 Jun 16;6(8):e1338236
B16F1 (murine melanoma cells)	35 µM	5-60 minutes	Evaluate the ability of LTX-315 to induce HMGB1 release from B16F1 cells, showing HMGB1 release within 30 minutes.	Cancer Immunol Immunother. 2014 Jun;63(6):601-13
U2OS osteosarcoma cells	12.5, 25, 50 μg/ml	6 and 24 hours	Induction of calreticulin (CALR) exposure detected by immunofluorescence staining	Cell Death Dis. 2016 Mar 10;7(3):e2134
U2OS osteosarcoma cells	12.5 to 50 mg/ml	6 hours	Observed morphological changes in cells, including mitochondrial dilation	Cell Cycle. 2015;14(21):3506-12

C57BL/6 mice	Orthotopic HCC model	Intratumoral injection	0.5 mg	Repeated injections on days 3, 6, and 9 after initial treatment	Evaluate the inhibitory effect of LTX-315 plus anti-CTLA-4 antibody on residual tumors, results showed combined treatment significantly inhibited tumor growth and prolonged survival	Cell Death Dis. 2025 Apr 13;16(1):288
PVG rats	Rat fibrosarcoma model	Intratumoral injection	1 mg	Consecutive 4 days	To evaluate the antitumor effect of LTX-315 in vivo, results showed that LTX-315 treatment led to complete tumor regression and induced systemic immune responses.	Oncoimmunology. 2017 Jun 16;6(8):e1338236
Mice	B16F10 melanoma model	Intratumoral injection	1 mg in 50 µl Saline	Three consecutive days	LTX-315 significantly decreased B16F10 tumor burden and improved overall mouse survival	Cell Stress. 2019 Oct 14;3(11):348-360
Female Balb/C wild-type mice	4 T1 mammary fat pad model	Intratumorally	1 mg peptide/injection	Once a day for 2-3 consecutive days	Evaluate the antitumor effect of LTX-315 in combination with CAELYX?, showing significant tumor growth inhibition and complete regression in the majority of treated animals	Breast Cancer Res. 2019 Jan 22;21(1):9
C57BL/6J mice	B16F10 melanoma model	Intratumoral injection	1 mg/50 µl PBS/injection	3 consecutive daily injections	LTX-315 strongly inhibited tumor growth in WT mice, an effect that was partially lost in MyD88-/- mice, suggesting that MyD88 is involved in the therapeutic effects of LTX-315.	Front Immunol. 2024 Mar 13;15:1332922
C57BL/6 mice	B16F1 melanoma model	Intratumoral injection	1 mg/50 μl	Once daily for 3 consecutive days	Evaluate the therapeutic effect of LTX-315 on B16F1 melanoma, showing complete tumor regression in most animals (30/37) within 5 weeks post-treatment.	Cancer Immunol Immunother. 2014 Jun;63(6):601-13
Sprague-Dawley rats	Rat orthotopic HCC model	Intratumoral injection	1.0 mg LTX-315, 1 mg/kg liposomal doxorubicin	Single treatment, followed up for 14 days	To evaluate the therapeutic efficacy of RFH-enhanced LTX-315 and liposomal doxorubicin combination therapy in rat orthotopic HCC. Results showed that the triple combination treatment group (RFH+LTX-315+liposomal doxorubicin) exhibited the best outcomes in terms of tumor volume, necrosis rate, and immune cell infiltration.	J Immunother Cancer. 2022 Nov;10(11):e005619
New Zealand white rabbits	VX2 liver tumor model	Direct infusion through the prongs of the RF electrode into the tumor margin	2 mg or 4 mg	Single administration	To validate the therapeutic effect of LTX-315 on residual tumors after incomplete RFA. Results showed that the 4 mg LTX-315 group had the smallest tumor volume and complete tumor necrosis.	Cancers (Basel). 2022 Dec 11;14(24):6093
Balb/c mice	4T1 breast tumor model	Intravenous injection	20 mg/kg LTX-315 and 1 mg/kg siRNA	Every 3 days for a total of 5 treatments	To evaluate the antitumor efficacy and immunomodulatory effects of LTX/siR-NPs in vivo. Results showed that LTX/siR-NPs significantly inhibited tumor growth, increased infiltration of CD8+ T cells and NK cells into tumors, and reduced the number of immunosuppressive cells.	Bioeng Transl Med. 2022 Aug 11;8(5):e10392
C57BL/6 mice	MCA205 sarcoma model	Intratumoral injection	300 μg	Three consecutive daily injections	LTX-315 rapidly reprograms the tumor microenvironment by decreasing the local abundance of immunosuppressive Tregs and myeloid-derived suppressor cells and by increasing the frequency of polyfunctional T helper type 1/type 1 cytotoxic T cells with a concomitant increase in cytotoxic T-lymphocyte antigen-4 (CTLA4) and drop in PD-1 expression levels. In tumors resistant to intratumoral or systemic CTLA4 blockade, subsequent local inoculation of LTX-315 cured the animals or caused tumor regressions with abscopal effects.	Cell Death Differ. 2016 Jun;23(6):1004-15
C57Bl/6 mice	MCA205 fibrosarcoma model	Intratumoral injection	300 μg	Single injection, observed after 1 and 4 days	LTX-315 induced local hemorrhagic necrosis accompanied by massive HMGB1 release and immune cell infiltration	Cell Death Dis. 2016 Mar 10;7(3):e2134
BALB/cAnN mice	TS/A mammary adenocarcinoma model	Intratumoral	300 μg	Once daily for 3 consecutive days	To evaluate the therapeutic effects of LTX-315 alone or in combination with radiotherapy on TS/A mammary adenocarcinoma. Results showed that LTX-315 slightly reduced the growth of primary tumors, and the effect was more pronounced when combined with radiotherapy.	Oncoimmunology. 2021 Aug 10;10(1):1962592

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CAS No.: 1345407-05-7

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CAS No.: 1345407-05-7

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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