Sitravatinib

• Description :

  Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively[1]. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment[2].

• Product Name Alternative :

  MGCD516; MG-516

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  C-Kit; Discoidin Domain Receptor; FLT3; Trk Receptor; VEGFR

• Type :

  Reference compound

• Related Pathways :

  Neuronal Signaling; Protein Tyrosine Kinase/RTK

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer; Inflammation/Immunology

• Assay Protocol :

  https://www.medchemexpress.com/Sitravatinib.html

• Purity :

  99.57

• Solubility :

  DMSO : ≥ 32 mg/mL

• 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

• Molecular Formula :

  C33H29F2N5O4S

• Molecular Weight :

  629.68

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Patwardhan PP 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, 2016 Jan 26;7 (4) :4093-109.|[2]Du W, et al. Sitravatinib potentiates immune checkpoint blockade in refractory cancer models. JCI Insight. 2018 Nov 2;3 (21) . pii: 124184.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 3

• Isoform :

  DDR1; DDR2; TrkA; TrkB; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4

• CAS Number :

  [1123837-84-2]