GLPBio

Sitravatinib

Catalog No.: GC19332Purity:>99.50%Synonyms: MGCD-516
COASDSData Sheet
Sitravatinib (MGCD516) ist ein oral bioverfÜgbarer Rezeptortyrosinkinase (RTK)-Inhibitor mit IC50-Werten von 1,5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0,5 nM, 29 nM, 5 nM und 9 nM fÜr Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA bzw. TRKB.

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Sitravatinib
Cas No.: 1123837-84-2
5mgIn Stock
$43.00
1
10mgIn Stock
$67.00
1
50mgIn Stock
$193.00
1
100mgIn Stock
$305.00
1
200mgIn Stock
$490.00
1
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Zitate (Citations)

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    Nature
    641, 529–536 (2025)
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    Nature
    628, 630–638 (2024)
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    Nature
    632, 686–694 (2024)
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    Nature
    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    Science
    388(6745) (2025)
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    387(6739) (2025)
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    387(6734) (2025)
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    35, 97–116 (2025)
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    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

Beschreibung (Description)

Sitravatinib is a tyrosine kinase inhibitor (TKI) that targets the TYRO3, AXL, and MERTK (TAM) receptors, the vascular endothelial growth factor receptor (VEGFR) family, c-Kit, and c-MET[1,2].

In vitro，Sitravatinib treatment decreased MET, EphA2, EphA3, or AXL protein phosphorylation levels in sunitinib and axitinib-resistant (SuR/AxR) human LM2-4 and mouse RENCA or 4T1 cells after 3 hours, enhanced effect in resistant cell lines[2]. The IC50 values for the three sensitive cell lines (DDLS, MPNST and LS141) ranged between 250–750nM, IC50 values for the less sensitive cell lines (A673 and Saos2) ranged between 1.5–2.0mM[3].

In vivo, Sitravatinib (2mg/kg; oral; every other day for 14 days) alone had 37% inhibitory effect on tumor volume (IRV) and 28% inhibitory effect on tumor weight (IRW) in the SW620 mice[4]. Sitravatinib (p.o.; 20mg/kg; once per day for 24 days) significantly inhibited tumor progression and induced tumor regression in immunocompetent mice bearing KLN205, CT1B-A5, or E0771 tumors[5].

References:
[1] Msaouel, Pavlos, et al. "Sitravatinib in combination with nivolumab plus ipilimumab in patients with advanced clear cell renal cell carcinoma: a phase 1 trial." Nature communications 16.1 (2025): 578.
[2] Dolan, Melissa, et al. "Enhanced efficacy of sitravatinib in metastatic models of antiangiogenic therapy resistance." PloS one 14.8 (2019): e0220101.
[3] Patwardhan, Parag P., et al. "Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma." Oncotarget 7.4 (2015): 4093.
[4] Yang, Yuqi, et al. "Modulating the function of ABCB1: in vitro and in vivo characterization of sitravatinib, a tyrosine kinase inhibitor." Cancer Communications 40.7 (2020): 285-300.
[5] Du, Wenting, et al. "Sitravatinib potentiates immune checkpoint blockade in refractory cancer models." JCI insight 3.21 (2018): e124184.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

Sunitinib and axitinib-resistant (SuR/AxR) human LM2-4 and mouse RENCA or 4T1 cells

Preparation Method

5x103 and 1x103 cells/well (for human and mouse SuR/AxR cell lines, respectively) were plated in 96-well plates in growth media. The next day, growth media was removed and replaced with media containing various concentrations of sitravatinib or cabozantinib. Sitravatinib concentrations ranged between 1 and 10μM for human and 0.02 and 10μM for mouse cell lines, and cabozantinib concentrations ranged between 0.01 and 10μM for mouse cell lines. Preliminary studies were conducted using multiple concentration ranges to arrive at optimal concentrations for IC50 determination. After 72 hours, MTS was added to the cells and, after 2 hours, measured at a wavelength of 490nm using a spectrophotometer.

Reaction Conditions

1 and 10μM for human and 0.02 and 10μM for mouse cell lines; 72 hours

Applications

Sitravatinib drug concentrations needed to reach 50% inhibition (IC50) was consistently less in SuR/AxR cells.
Animal experiment [2]:

Animal models

SW620 and SW620/Ad300 cells transplanted nude mice

Preparation Method

SW620 and SW620/Ad300 cells were harvested and washed twice with PBS. Then, both cell lines (1×107 cells in 0.1mL PBS) were injected subcutaneously under armpits of the nude mice. Once the tumor volume reached 500mm3, the mice were euthanized, and the tumor tissues were dissected. Each tumor tissue, except the necrotic part, was cut into 2×2mm in size. The small tumor pieces were implanted subcutaneously under armpits of the nude mice. When the tumor reached approximately 100mm3, the mice were randomly assigned to the following four groups. Sitravatinib was prepared in a final concentration of 0.5% hydroxypropyl methylcellulose (HPMC) and 0.1% Tween-80 solution (pH 1.4) (vehicle A), while vincristine was prepared in autoclaved water (vehicle B). Group 1 mice received vehicle A (administered orally) 1h prior to vehicle B (administered intraperitoneally). Group 2 mice received sitravatinib (prepared in vehicle A, 2mg/kg, administered orally) 1h prior to vehicle B (administered intraperitoneally). Group 3 mice received vehicle A (administered orally) 1h prior to vincristine (prepared in vehicle B, 0.4mg/kg, administered intraperitoneally). Group 4 mice received sitravatinib 1h prior to vincristine at indicated dosages. All treatments were given every other day for 14 days.

Dosage form

2mg/kg; oral; every other day for 14 days.

Applications

Sitravatinib alone had 37% inhibitory effect on tumor volume (IRV) and 28% inhibitory effect on tumor weight (IRW) compared with the control group treated with vehicle only in the SW620 mice. The growth of xenograft tumors was significantly inhibited by combination of sitravatinib and vincristine with 76% IRV and 89% IRW.

References:
[1]. Dolan, Melissa, et al. "Enhanced efficacy of sitravatinib in metastatic models of antiangiogenic therapy resistance." PloS one 14.8 (2019): e0220101.
[2]. Yang, Yuqi, et al. "Modulating the function of ABCB1: in vitro and in vivo characterization of sitravatinib, a tyrosine kinase inhibitor." Cancer Communications 40.7 (2020): 285-300.

Produktdokumente (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
1123837-84-2
Synonyme
MGCD-516
SMILES
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
Summenformel
C33H29F2N5O4S
Molekulargewicht
629.68
Löslichkeit
DMSO : ≥ 32 mg/mL (50.82 mM)
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

Reviews

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