Sitravatinib (MGCD516) | RTK Inhibitor

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CAS No. :	1123837-84-2
Formula :	C₃₃H₂₉F₂N₅O₄S
M.W :	629.68
SMILES Code :	O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=C5C(C=C(C6=NC=C(CNCCOC)C=C6)S5)=NC=C4)C(F)=C3
Synonyms :	MGCD516; MG-516
MDL No. :	MFCD28502181
InChI Key :	WLAVZAAODLTUSW-UHFFFAOYSA-N
Pubchem ID :	25212148

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

NCI-H460/MX20	3 µM	72 hours	Restore the antineoplastic effect of ABCG2 substrates	PMC7236772
HEK293/ABCG2-482-R2	3 µM	72 hours	Restore the antineoplastic effect of ABCG2 substrates	PMC7236772
S1-M1-80	3 µM	72 hours	Restore the antineoplastic effect of ABCG2 substrates	PMC7236772
Res1-6 cells	0, 0.1, 0.5, 1.0, 2.0, 4.0, 8.0, 16.0, and 32.0 μM		Assess cell survival rate under coculture conditions, finding that Hepa1-6-OE-MerTK cells showed increased survival rate over time	PMC10897610
Ba/F3 cells	100 nM	72 hours	Screening for drugs active against D1228X or Y1230X secondary mutations, revealing that Sitravatinib and other four type II MET-TKIs inhibited growth by less than 50% in D1228A/Y mutant cells.	PMC9188708
Saos2	1.5–2.0 μmol/L	72 hours	MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects	PMC4826192
A673	1.5–2.0 μmol/L	72 hours	MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects	PMC4826192
MPNST	250-750 nmol/L	72 hours	MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects	PMC4826192
LS141	250-750 nmol/L	72 hours	MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects	PMC4826192
DDLS	250-750 nmol/L	72 hours	MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects	PMC4826192
BaF3-FLT3-ITD-F691L cells	3 nM	4 hours	Evaluate the inhibitory effect of Sitravatinib on BaF3-FLT3-ITD-F691L cell signaling pathways, results showed Sitravatinib effectively inhibited the signaling pathways of FLT3-ITD-F691L mutant cells	PMC9872318
MOLM13 cells	1.511 nM	48 hours	Evaluate the inhibitory effect of Sitravatinib on MOLM13 cell proliferation, results showed Sitravatinib significantly inhibited the proliferation of FLT3-ITD AML cell lines	PMC9872318
MV4-11 cells	0.556 nM	48 hours	Evaluate the inhibitory effect of Sitravatinib on MV4-11 cell proliferation, results showed Sitravatinib significantly inhibited the proliferation of FLT3-ITD AML cell lines	PMC9872318
HEK293/ABCC10 cells	3 µmol/L	72 hours	Evaluate the reversal effect of Sitravatinib on ABCC10-mediated multidrug resistance, results showed that Sitravatinib partially reversed the resistance of HEK293/ABCC10 cells to paclitaxel	PMC7365458
HEK293/ABCB1 cells	3 µmol/L	72 hours	Evaluate the reversal effect of Sitravatinib on ABCB1-mediated multidrug resistance, results showed that Sitravatinib significantly reduced the IC50 values of paclitaxel, doxorubicin, and vincristine in HEK293/ABCB1 cells	PMC7365458
SW620/Ad300 cells	3 µmol/L	72 hours	Evaluate the reversal effect of Sitravatinib on ABCB1-mediated multidrug resistance, results showed that Sitravatinib significantly reduced the IC50 values of paclitaxel, doxorubicin, and vincristine in SW620/Ad300 cells	PMC7365458
KB-C2 cells	3 µmol/L	72 hours	Evaluate the reversal effect of Sitravatinib on ABCB1-mediated multidrug resistance, results showed that Sitravatinib significantly reduced the IC50 values of paclitaxel, doxorubicin, and vincristine in KB-C2 cells	PMC7365458
Bone marrow-derived macrophages (BMDMs)	12.5, 50, 200, 800 nM	2 hours (LPS stimulation) or 18 hours (IL-4 stimulation)	Sitravatinib dose-dependently inhibited the IL-4 plus CM–mediated expression of Arg1, Ym-1, and Fizz1, markers associated with an immunosuppressive macrophage phenotype, but did not affect the LPS plus CM–induced expression of Tnfα, Il-6, or Il-12, markers of an immunostimulatory macrophage phenotype.	PMC6238734
Bone marrow–derived macrophages (BMDMs)	12.5, 50, 200, 800 nM	2 hours (LPS) or 18 hours (IL-4)	To evaluate the effect of sitravatinib on macrophage polarization. Results showed that sitravatinib dose-dependently inhibited the IL-4 plus CM–mediated expression of Arg1, Ym-1, and Fizz1 (markers associated with an immunosuppressive macrophage phenotype) but did not affect the LPS plus CM–induced expression of Tnfα, Il-6, or Il-12 (markers of an immunostimulatory macrophage phenotype).	PMC6238734

NSG mice	MOLM13 xenograft model	Oral gavage	20 mg/kg	Once daily for 14 days	Evaluate the anti-tumor effect of Sitravatinib in the MOLM13 xenograft model, results showed Sitravatinib significantly prolonged the survival time of mice	PMC9872318
C57BL/6 mice	Subcutaneous Hepa1-6 tumor model	Oral	20 mg/kg	6 days per week for 25 days	Evaluate the antitumor effect of sitravatinib combined with anti-PD-L1 antibody, finding that the combination therapy significantly inhibited tumor growth	PMC10897610
Crl:NU(NCr)-Foxn1nu nude mice	TNBC xenograft model	Oral	10 mg/kg/day	Continuous treatment: 6 days a week for several weeks; Alternating treatment: two days single drug, two days combined, two days single drug.	Evaluate the efficacy of Sitravatinib combined with Abemaciclib in TNBC xenograft models, showing significant suppression of tumor growth.	PMC11202171
ICR/SCID mice	MPNST and LS141 xenograft models	Oral	15 mg/kg	Once daily, 5 days a week for 3 weeks	MGCD516 treatment resulted in significant suppression of tumor growth compared to vehicle control as well as compared against imatinib and crizotinib	PMC4826192
Mice	KLN205, CT1B-A5, and E0771 tumor models	Oral	20 mg/kg	Once daily for 6 days or 2.5 weeks	Sitravatinib significantly inhibited tumor progression and induced tumor regression, reduced the number of tumor-associated immunosuppressive myeloid cells, increased the number of CD4+ T cells and exhausted CD8+ T cells, and enhanced the efficacy of PD-1 blockade.	PMC6238734
Nude mice	SW620/Ad300 xenograft model	Oral administration	2 mg/kg	Every other day for 14 days	Evaluate the reversal effect of Sitravatinib combined with vincristine on ABCB1-mediated multidrug resistance, results showed that the combination therapy significantly inhibited the growth of SW620/Ad300 xenograft tumors	PMC7365458

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CAS No.: 1123837-84-2

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CAS No.: 1123837-84-2

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NCT02978859	Liposarcoma\|Metastatic Liposar... More >>coma Less <<	PHASE2	COMPLETED	2021-12-20	Massachussetts General Hospita... More >>l, Boston, Massachusetts, 02114-2696, United States\|Washington University, Saint Louis, Missouri, 63130, United States\|Columbia University Irving Medical Center, New York, New York, 10032, United States Less <<
NCT04123704	Breast Cancer Stage IV\|Triple ... More >>Negative Breast Cancer\|Breast Neoplasms\|Breast Cancer Metastatic Less <<	PHASE2	TERMINATED	2023-01-22	Baylor College of Medicine, Ho... More >>uston, Texas, 77030, United States Less <<
NCT02219711	Advanced Cancer	PHASE1	COMPLETED	2022-04-27	University of Alabama, Birming... More >>ham, Alabama, 35294, United States\|University of California, San Diego, San Diego, California, 92093, United States\|University of California, San Francisco, San Francisco, California, 94143, United States\|Sarcoma Oncology Research Center, Santa Monica, California, 90403, United States\|Innovative Clinical Research Institute, Whittier, California, 90602, United States\|Rocky Mountain Cancer Center, Denver, Colorado, 80218, United States\|Holy Cross Michael & Dianne Bienes Comprehensive Cancer Center, Fort Lauderdale, Florida, 33308, United States\|Florida Cancer Affiliates, Ocala, Florida, 34471, United States\|Florida Cancer Specialists, Sarasota, Florida, 34232, United States\|Northwestern University, Chicago, Illinois, 60611, United States\|Rush University Medical Center, Chicago, Illinois, 60612, United States\|Ochsner Clinic Foundation, New Orleans, Louisiana, 70121, United States\|Maryland Oncology Hematology,, Rockville, Maryland, 20850, United States\|Massachusetts General Hospital, Boston, Massachusetts, 02114, United States\|University of Michigan, Ann Arbor, Michigan, 48109, United States\|Henry Ford Health System, Detroit, Michigan, 48202, United States\|Washington University Center for Advanced Medicine, Saint Louis, Missouri, 63110, United States\|CHI Health St Francis, Saint Francis Cancer Treatment Center, Grand Island, Nebraska, 68803, United States\|Oncology Hematology West PC, Nebraska Cancer Specialists, Omaha, Nebraska, 68130, United States\|University of New Mexico Cancer Research and Treatment Center, Albuquerque, New Mexico, 87102, United States\|Montefiore Medical Center, Bronx, New York, 10467, United States\|Roswell Park Cancer Institute, Buffalo, New York, 14263, United States\|Columbia University, New York, New York, 10032, United States\|Oncology Hematology Care, Inc., Cincinnati, Ohio, 45242, United States\|Guthrie Clinical Research, Sayre, Pennsylvania, 18840, United States\|St. Francis Cancer Center, Greenville, South Carolina, 29607, United States\|Sarah Cannon Research Institute, Nashville, Tennessee, 37203, United States\|Texas Oncology-Austin Midtown, Austin, Texas, 78705, United States\|Mary Crowley Cancer Research Center, Dallas, Texas, 75251, United States\|University of Texas, MD Anderson Cancer Center, Houston, Texas, 77030, United States\|Texas Oncology-Tyler, Tyler, Texas, 75702, United States\|The Huntsman Cancer Institute, Salt Lake City, Utah, 84112, United States\|Virginia Cancer Specialists, Fairfax, Virginia, 22031, United States\|Oncology and Hematology Associates of Southwest Virginia, Inc., Blue Ridge Cancer Care, Roanoke, Virginia, 24014, United States\|Seattle Cancer Care Alliance, Seattle, Washington, 98109, United States\|Northwest Cancer Specialists, P.C., Vancouver, Washington, 98684, United States\|University of Wisconsin, Madison, Wisconsin, 53792, United States\|Chungbuk National University Hospital, Cheongju-si, Korea, Republic of\|Keimyung University Dongsan Hospital, Daegu, Korea, Republic of\|National Cancer Center, Goyang-si, Korea, Republic of\|Korea Veterans Health Service, Seoul, Korea, Republic of\|Seoul National University Hospital, Seoul, Korea, Republic of\|Severance Hospital, Yonsei University Health System, Seoul, Korea, Republic of Less <<

Bio Calculators
Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	1.59mL 0.32mL 0.16mL	7.94mL 1.59mL 0.79mL	15.88mL 3.18mL 1.59mL
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