Ligritinib
Based on 1 Customer Validation
Ligritinib (AB801) is an orally active AXL receptor tyrosine kinase inhibitor, with a IC50 of 1.8 nM, Ki of 0.024 nM, and Kd of 0.093 nM against human targets. It exhibits broad selectivity against the human kinome, including high selectivity for MERTK and TYRO3. Ligritinib blocks the AXL signaling pathway independent of dimerization inducers, and acts as both a tumor growth inhibitor and an AXL inducer. Ligritinib can be used in research related to clear cell renal cell carcinoma, advanced solid tumors, and non-small cell lung cancer.
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- Pureza: 98.08%
- No. CAS: 3024588-48-2
- Fòrmula: C33H32N6O
- Peso molecular:528.65
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Actividad biológica
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Axl 1.8 nM (IC50) |
Axl 0.024 nM (Ki) |
Axl 0.093 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | IC50 |
68 nM
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Inhibition of AXL autophosphorylation in transiently transfected human HEK293T cells incubated for 1 h in 100% human serum, measured via pAXL ELISA with NanoLuc activity readout.
Inhibition of AXL autophosphorylation in transiently transfected human HEK293T cells incubated for 1 h in 100% human serum, measured via pAXL ELISA with NanoLuc activity readout.
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40407274 |
Ligritinib (1 h) inhibits the autophosphorylation of AXL in transiently transfected HEK293T cells, with an IC50 of 68 nM in 100% human serum[1].
Ligritinib (10 μM) inhibits hERG channels by 46%[1].
Ligritinib exhibits limited direct inhibitory effects on human CYP isoenzymes, with its IC50 values ranging from 5.6 μM (CYP3A4-T) to >100 μM (CYP1A2, CYP2B6)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nu/Nu (female, 6-10 weeks old, human clear-cell renal cell carcinoma 786-O xenograft model via subcutaneous injection of 4 × 106 cells in right flank)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; daily
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Result:Did not result in tumor growth inhibition compared to vehicle control when administered as single-agent at 10 mg/kg or 30 mg/kg.
Caused a statistically significant reduction in tumor volume compared to vehicle, single-agent sunitinib, or single-agent Ligritinib when combined with Sunitinib at 30 mg/kg.
Showed statistically significant tumor growth inhibition compared to vehicle control but not compared to single-agent Sunitinib or Ligritinib when combined with sunitinib at 10 mg/kg.
Significantly increased plasma levels of soluble AXL at 30 mg/kg, indicative of AXL inhibition.
Was well-tolerated, with no significant loss of body weight observed.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 3024588-48-2
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Appearance Solid
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Peso molecular 528.65
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Fòrmula C33H32N6O
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Color Off-white to pink
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SMILES
CC(C=CC=N1)=C1C(C=N2)=CC=C2C3=NNC4=NC=C(C=C43)C5=CC6=C(C=C5)CC[C@@H](CC6)N7C8COCC7C8
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Synonyms
AB801
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ligritinib Related Classifications
HY-176205 Related Classifications
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