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

Product Name: 1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]-
CAS No.: 2367004-54-2
Chemical Name: 1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]-
Synonyms: XL-092;JUN04542;Zanzalintinib;XL092, 10 mM in DMSO;Zanzalintinib (XL-092);N-(4-Fluorophenyl)-N-(4-((7-methoxy-6-(methylcarbamoyl)quinolin-4-yl)oxy)phenyl)cyclopropane-1,1-dicarboxamide;1-N'-(4-fluorophenyl)-1-N-[4-[7-methoxy-6-(methylcarbamoyl)quinolin-4-yl]oxyphenyl]cyclopropane-1,1-dicarboxamide;1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]-;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
CBNumber: CB98845693
Molecular Formula: C29H25FN4O5
Formula Weight: 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]- Property

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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Hazard and Precautionary Statements (GHS)

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

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 T_1/2 of 5.4 hours, a CL of 43 mL/hr kg. Zanzalintinib (3 mg/kg; po) has a T_1/2 of 7.1 hours and a C_max of 11.4 μM for rats^[2].

Animal Model:	Rat^[1]
Dosage:	3 mg/kg (Pharmacokinetic Analysis)
Administration:	IV
Result:	Had a T_1/2 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]- Preparation Products And Raw materials

Raw materials

Preparation Products

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

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2367004-54-2, 1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]-Related Search:

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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

1-N'-(4-fluorophenyl)-1-N-[4-[7-methoxy-6-(methylcarbamoyl)quinolin-4-yl]oxyphenyl]cyclopropane-1,1-dicarboxamide

2367004-54-2