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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- 純度: 98.08%
- CAS 番号: 3024588-48-2
- 分子式: C33H32N6O
- 分子量:528.65
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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 |
|---|---|---|---|---|
| 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 |
化学情報
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CAS 番号 3024588-48-2
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性状 Solid
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分子量 528.65
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分子式 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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別名
AB801
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Ligritinib 関連分類
HY-176205 関連分類
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