Axl

Axl製品

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  • Axl阻害剤 (22)
  • Axl抗体(3)
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S1119 Cabozantinib (XL184) カボザンチニブ (Cabozantinib (XL184, BMS-907351)) は強力な VEGFR2 阻害剤であり、IC50 は 0.035 nM です。また c-Met, Ret, Kit, Flt-1/3/4, Tie2 および AXL に対しても阻害活性があり、cell-free assay における IC50 はそれぞれ 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM, 7 nM です。カボザンチニブは大腸がん細胞において AKT/GSK-3β/NF-κB 経路を介して PUMA 依存性アポトーシス (PUMA-dependent apoptosis) を誘発します。
Front Immunol, 2024, 15:1258475
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
S2841 Bemcentinib (R428) ベムセンチニブ (Bemcentinib (R428、BGB324)) は Axl の阻害剤 (IC50 =14 nM) であり、Abl に比べて 100 倍以上の選択性を持ちます。 Mer および Tyro3 (50 ~ 100 倍) および InsR, EGFR, HER2および PDGFRβ に対しても高い Axl 選択性 (100 倍) を示します。
Nat Commun, 2024, 15(1):2818
Nat Commun, 2024, 15(1):6344
Theranostics, 2024, 14(7):2656-2674
S4001 Cabozantinib malate Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
Cancer Sci, 2023, 114(4):1651-1662
Cancer Sci, 2023, 114(4):1651-1662
S1561 BMS-777607 BMS-777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases.
Cancer Lett, 2024, 587:216692
Nat Commun, 2023, 14(1):4162
Oncogene, 2023, 42(21):1716-1727
S7754 Gilteritinib (ASP2215) Gilteritinib (ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).
Front Immunol, 2024, 15:1200461
Mol Oncol, 2024, 10.1002/1878-0261.13749
Commun Biol, 2024, 7(1):412
S7846 Dubermatinib(TP-0903) TP-0903 is a potent and selective AXL Inhibitor with IC50 of 27 nM. TP-0903 is highly effective in inducing apoptosis.
Mol Oncol, 2024, 10.1002/1878-0261.13749
Cell Rep, 2023, 42(9):113067
Sci Adv, 2022, 8(20):eabk2746
S7638 LDC1267 LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8.
Cell Metab, 2021, S1550-4131(21)00326-0
J Clin Invest, 2021, 131(8)e139434 139434
J Clin Invest, 2021, 131(8)139434
S7576 UNC2025 HCl UNC-2025 HCl is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.
Immunity, 2023, 56(8):1778-1793.e10
Cell Rep, 2022, 38(13):110600
Cancers (Basel), 2021, 13(23)6072
S7014 Merestinib (LY2801653) Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.
NPJ Breast Cancer, 2024, 10(1):65
Cancers (Basel), 2024, 16(12)2253
J Clin Invest, 2021, 131(11)146987
S9662 UNC2025 UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively.
iScience, 2024, 27(7):110226
Commun Biol, 2023, 6(1):916
Commun Biol, 2023, 6(1):916
S8570 CEP-40783 (RXDX-106) CEP-40783 (RXDX-106) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively.
bioRxiv, 2023, 2023.10.20.563266
Mol Cancer Res, 2022, 20(4):542-555
J Oncol, 2022, 2022:2946929
S8573 Sitravatinib (MGCD516) Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
JCI Insight, 2022, e148717
Cancers (Basel), 2021, 13(21)5474
Cancers (Basel), 2020, 12(1)
S7847 SGI-7079 SGI-7079 ,a novel selective Axl inhibitor, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.
Blood Cancer J, 2021, 11(5):93
Clin Cancer Res, 2017, 23(11):2713-2722
Oncotarget, 2017, 8(52):89761-89774
S7669 NPS-1034 NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.
Nat Commun, 2023, 14(1):4162
J Med Chem, 2021, 64(6):3165-3184
Sci Rep, 2021, 11(1):19667
S7325 UNC2881 UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively.
Cell Rep, 2020, 30(11):3671-3681
Front Immunol, 2019, 10:2647
S8404 S49076 S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.
Mol Brain, 2020, 4;13(1):66
S8933 Tamnorzatinib (ONO-7475) Tamnorzatinib (ONO-7475) is a potent, selective, and orally active novel inhibitor of Anexelekto(Axl)/MER tyrosine kinase with IC50 of 0.7 nM and 1.0 nM for AXL and MER, respectively. ONO-7475 suppresses the emergence and maintenance of tolerant cells to the initial EGFR-TKIs, osimertinib or dacomitinib, in AXL-overexpressing EGFR-mutated NSCLC cells. ONO-7475 arrests growth and kills FMS-like tyrosine kinase 3-internal tandem duplication mutant acute myeloid leukemia cells.
Cancer Lett, 2024, 587:216692
Cancer Sci, 2024, 10.1111/cas.16292
JTO Clin Res Rep, 2023, 4(6):100525
A2596 Tilvestamab (Anti-AXL / UFO) Tilvestamab (Anti-AXL / UFO) is a humanized antibody targeting AXL.Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas. MW :146.16 KD.
S0071 RU-301 RU-301 is a pan-TAM receptor (Axl, Tyro3 and Mertk) inhibitor that blocks the Axl receptor dimerization site with Kd of 12 μM and IC50 of 10 μM, respectively.
S6870 Ningetinib Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. Ningetinib exhibits antitumor activity.
E1818New PF-07265807 PF-07265807(TAM&Met-IN-1) is a dual inhibitor of AXL and MER, which exhibits anti-tumor effects. It also enhances the function of dendritic cells to cross-prime CD8+ T cells.
A2586 Enapotamab (Anti-AXL / UFO) Enapotamab(Anti-AXL / UFO) is a highly specific rabbit polyclonal antibody that targets receptor tyrosine kinase AXL (UFO). It demonstrates potent activity in immunotherapeutic strategy for the treatment of sarcomas. MW :145.42 KD.
A2774 Mipasetamab (Anti-AXL / UFO) Mipasetamab (Anti-AXL / UFO) is a human monoclonal IgG1κ antibody targeting AXL, a tyrosine kinase receptor, and an TAM receptor, which involves the synthesis of ADCT-601 (Mipasetamab uzoptirine), an AXL-targeted antibody-drug conjugate (ADC). MW: 145.78 kD.
D4038New Enapotamab vedotin Enapotamab vedotin (EnaV, HuMAX-AXL-ADC) is an AXL-specific human IgG1 antibody conjugated to the microtubule disrupting agent monomethyl auristatin E (MMAE) through a protease cleavable valine-citrulline (vc) linker.
E0142 XL092 XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.
S1119 Cabozantinib (XL184) カボザンチニブ (Cabozantinib (XL184, BMS-907351)) は強力な VEGFR2 阻害剤であり、IC50 は 0.035 nM です。また c-Met, Ret, Kit, Flt-1/3/4, Tie2 および AXL に対しても阻害活性があり、cell-free assay における IC50 はそれぞれ 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM, 7 nM です。カボザンチニブは大腸がん細胞において AKT/GSK-3β/NF-κB 経路を介して PUMA 依存性アポトーシス (PUMA-dependent apoptosis) を誘発します。
Front Immunol, 2024, 15:1258475
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
S2841 Bemcentinib (R428) ベムセンチニブ (Bemcentinib (R428、BGB324)) は Axl の阻害剤 (IC50 =14 nM) であり、Abl に比べて 100 倍以上の選択性を持ちます。 Mer および Tyro3 (50 ~ 100 倍) および InsR, EGFR, HER2および PDGFRβ に対しても高い Axl 選択性 (100 倍) を示します。
Nat Commun, 2024, 15(1):2818
Nat Commun, 2024, 15(1):6344
Theranostics, 2024, 14(7):2656-2674
S4001 Cabozantinib malate Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
Cancer Sci, 2023, 114(4):1651-1662
Cancer Sci, 2023, 114(4):1651-1662
S1561 BMS-777607 BMS-777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases.
Cancer Lett, 2024, 587:216692
Nat Commun, 2023, 14(1):4162
Oncogene, 2023, 42(21):1716-1727
S7754 Gilteritinib (ASP2215) Gilteritinib (ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).
Front Immunol, 2024, 15:1200461
Mol Oncol, 2024, 10.1002/1878-0261.13749
Commun Biol, 2024, 7(1):412
S7846 Dubermatinib(TP-0903) TP-0903 is a potent and selective AXL Inhibitor with IC50 of 27 nM. TP-0903 is highly effective in inducing apoptosis.
Mol Oncol, 2024, 10.1002/1878-0261.13749
Cell Rep, 2023, 42(9):113067
Sci Adv, 2022, 8(20):eabk2746
S7638 LDC1267 LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8.
Cell Metab, 2021, S1550-4131(21)00326-0
J Clin Invest, 2021, 131(8)e139434 139434
J Clin Invest, 2021, 131(8)139434
S7576 UNC2025 HCl UNC-2025 HCl is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.
Immunity, 2023, 56(8):1778-1793.e10
Cell Rep, 2022, 38(13):110600
Cancers (Basel), 2021, 13(23)6072
S7014 Merestinib (LY2801653) Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.
NPJ Breast Cancer, 2024, 10(1):65
Cancers (Basel), 2024, 16(12)2253
J Clin Invest, 2021, 131(11)146987
S9662 UNC2025 UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively.
iScience, 2024, 27(7):110226
Commun Biol, 2023, 6(1):916
Commun Biol, 2023, 6(1):916
S8570 CEP-40783 (RXDX-106) CEP-40783 (RXDX-106) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively.
bioRxiv, 2023, 2023.10.20.563266
Mol Cancer Res, 2022, 20(4):542-555
J Oncol, 2022, 2022:2946929
S8573 Sitravatinib (MGCD516) Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
JCI Insight, 2022, e148717
Cancers (Basel), 2021, 13(21)5474
Cancers (Basel), 2020, 12(1)
S7847 SGI-7079 SGI-7079 ,a novel selective Axl inhibitor, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.
Blood Cancer J, 2021, 11(5):93
Clin Cancer Res, 2017, 23(11):2713-2722
Oncotarget, 2017, 8(52):89761-89774
S7669 NPS-1034 NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.
Nat Commun, 2023, 14(1):4162
J Med Chem, 2021, 64(6):3165-3184
Sci Rep, 2021, 11(1):19667
S7325 UNC2881 UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively.
Cell Rep, 2020, 30(11):3671-3681
Front Immunol, 2019, 10:2647
S8404 S49076 S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.
Mol Brain, 2020, 4;13(1):66
S8933 Tamnorzatinib (ONO-7475) Tamnorzatinib (ONO-7475) is a potent, selective, and orally active novel inhibitor of Anexelekto(Axl)/MER tyrosine kinase with IC50 of 0.7 nM and 1.0 nM for AXL and MER, respectively. ONO-7475 suppresses the emergence and maintenance of tolerant cells to the initial EGFR-TKIs, osimertinib or dacomitinib, in AXL-overexpressing EGFR-mutated NSCLC cells. ONO-7475 arrests growth and kills FMS-like tyrosine kinase 3-internal tandem duplication mutant acute myeloid leukemia cells.
Cancer Lett, 2024, 587:216692
Cancer Sci, 2024, 10.1111/cas.16292
JTO Clin Res Rep, 2023, 4(6):100525
S0071 RU-301 RU-301 is a pan-TAM receptor (Axl, Tyro3 and Mertk) inhibitor that blocks the Axl receptor dimerization site with Kd of 12 μM and IC50 of 10 μM, respectively.
S6870 Ningetinib Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. Ningetinib exhibits antitumor activity.
E1818New PF-07265807 PF-07265807(TAM&Met-IN-1) is a dual inhibitor of AXL and MER, which exhibits anti-tumor effects. It also enhances the function of dendritic cells to cross-prime CD8+ T cells.
D4038New Enapotamab vedotin Enapotamab vedotin (EnaV, HuMAX-AXL-ADC) is an AXL-specific human IgG1 antibody conjugated to the microtubule disrupting agent monomethyl auristatin E (MMAE) through a protease cleavable valine-citrulline (vc) linker.
E0142 XL092 XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.
A2596 Tilvestamab (Anti-AXL / UFO) Tilvestamab (Anti-AXL / UFO) is a humanized antibody targeting AXL.Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas. MW :146.16 KD.
A2586 Enapotamab (Anti-AXL / UFO) Enapotamab(Anti-AXL / UFO) is a highly specific rabbit polyclonal antibody that targets receptor tyrosine kinase AXL (UFO). It demonstrates potent activity in immunotherapeutic strategy for the treatment of sarcomas. MW :145.42 KD.
A2774 Mipasetamab (Anti-AXL / UFO) Mipasetamab (Anti-AXL / UFO) is a human monoclonal IgG1κ antibody targeting AXL, a tyrosine kinase receptor, and an TAM receptor, which involves the synthesis of ADCT-601 (Mipasetamab uzoptirine), an AXL-targeted antibody-drug conjugate (ADC). MW: 145.78 kD.
E1818New PF-07265807 PF-07265807(TAM&Met-IN-1) is a dual inhibitor of AXL and MER, which exhibits anti-tumor effects. It also enhances the function of dendritic cells to cross-prime CD8+ T cells.
D4038New Enapotamab vedotin Enapotamab vedotin (EnaV, HuMAX-AXL-ADC) is an AXL-specific human IgG1 antibody conjugated to the microtubule disrupting agent monomethyl auristatin E (MMAE) through a protease cleavable valine-citrulline (vc) linker.

Axl阻害剤の選択性比較

Tags: Axl inhibitor|Axl agonist|Axl activator|Axl inducer|Axl antagonist|Axl signaling pathway|Axl assay kit