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
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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
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 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/hrkg. |
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
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