Basic information Safety Supplier Related

1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]-

Basic information Safety Supplier Related

1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]- Basic information

Product Name:
1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]-
Synonyms:
  • 1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]-
  • XL-092
  • JUN04542
  • Zanzalintinib
  • Axl,c-Met/HGFR,Vascular endothelial growth factor receptor,p-MET,XL092,TAM Receptor,p-VEGFR2,Mer,ATP,XL 092,VEGFR,Inhibitor,Tyro3,XL-092,orally,inhibit
  • N-(4-Fluorophenyl)-N-(4-((7-methoxy-6-(methylcarbamoyl)quinolin-4-yl)oxy)phenyl)cyclopropane-1,1-dicarboxamide
  • Zanzalintinib (XL-092)
  • XL092, 10 mM in DMSO
CAS:
2367004-54-2
MF:
C29H25FN4O5
MW:
528.53
Mol File:
2367004-54-2.mol
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1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]- Chemical Properties

Boiling point:
840.4±65.0 °C(Predicted)
Density 
1.408±0.06 g/cm3(Predicted)
storage temp. 
4°C, protect from light
solubility 
DMSO : 25 mg/mL (47.30 mM; Need ultrasonic)
pka
13.14±0.46(Predicted)
form 
Solid
color 
Off-white to light brown
InChIKey
JSPCKALGNNVYOO-UHFFFAOYSA-N
SMILES
C1(C(NC2=CC=C(OC3C4C(N=CC=3)=CC(OC)=C(C(NC)=O)C=4)C=C2)=O)(C(NC2=CC=C(F)C=C2)=O)CC1
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1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]- Usage And Synthesis

Uses

Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research[1][2].

in vivo

Zanzalintinib (10 mg/kg/day; oral; for 14 days) causes substantial tumor growth inhibition in xenograft studies. Zanzalintinib shows 82% and 96% inhibition on p-MET and p-VEGFR2, respectively[1].
Zanzalintinib (compound 8; 3 mg/kg; iv) has a T1/2 of 5.4 hours, a CL of 43 mL/hr kg. Zanzalintinib (3 mg/kg; po) has a T1/2 of 7.1 hours and a Cmax of 11.4 μM for rats[2].

Animal Model:Rat[1]
Dosage:3 mg/kg (Pharmacokinetic Analysis)
Administration:IV
Result:Had a T1/2 of 5.4 hours, a CL of 43 mL/hr?kg.

IC 50

Axl; Mer; VEGFR2: 1.6 nM (IC50); AXL: 3.4 nM (IC50); MER: 7.2 nM (IC50)

References

[1] J. Hsu, et al. XL092, a multi-targeted inhibitor of MET, VEGFR2, AXL and MER with an optimized pharmacokinetic profile. European Journal of Cancer, Volume 138, Supplement 2, October 2020, Page S16.
[2] Lynne Canne Bannen, et al. Compounds for the treatment of kinase-dependent disorders. WO2019148044A1.

1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]-Supplier

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WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
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1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]-(2367004-54-2)Related Product Information