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TAM receptors (Tyro-3,Axl,and Mertk)
TAM receptors (Tyro-3,Axl,and Mertk)製品
- All (30)
- TAM receptors (Tyro-3,Axl,and Mertk)阻害剤 (28)
- TAM receptors (Tyro-3,Axl,and Mertk)抗体(2)
- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|---|
| 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。 |
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| 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。 |
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| 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. |
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|
| 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. |
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|
| 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). | ||
| 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. |
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|
| S1497 | Pralatrexate | Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis. |
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|
| S7342 | UNC2250 | UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3. |
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|
| S8696 | 2-D08 | 2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. | ||
| 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. |
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| S8619 | NCT-503 | NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with the IC50 value of 2.5 μM. It is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. |
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|
| S7669 | NPS-1034 | NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7545 | G-749 | G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, showing lower potency against other tyrosine kinases. | ||
| A2851 | Emactuzumab (Anti-CSF1R / M-CSFR / CD115) | Emactuzumab (Anti-CSF1R / M-CSFR / CD115) is a humanized monoclonal antibody directed against the tyrosine kinase receptor colony stimulating factor 1 receptor (CSF1R, CSF-1R, CD115), also known as macrophage colony-stimulating factor receptor (M-CSFR), with potential antineoplastic and immunomodulating activities MW : 146.94 KD. | ||
| 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. | ||
| E5942New | UNC9426 | UNC9426 (compound 12) is a potent and orally bioavailable inhibitor of TYRO3 with an IC50 of 2.1 nM. It reduces platelet aggregation without prolonging bleeding time and effectively suppresses TYRO3-mediated signalling pathways in tumor cells and macrophages. | ||
| 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. | ||
| E7462New | Merestinib dihydrochloride | メレスチニブ二塩酸塩（LY2801653二塩酸塩）は、強力で経口投与可能なc - Met阻害剤（Ki = 2 nM）で、抗腫瘍活性を有しています。メレスチニブ二塩酸塩は、MST1R（IC50 = 11 nM）、FLT3（IC50 = 7 nM）、AXL（IC50 = 2 nM）、MERTK（IC50 = 10 nM）、TEK（IC50 = 63 nM）、ROS1、DDR1/2（IC50 = 0.1/7 nM）およびMKNK1/2（IC50 = 7 nM）に対しても強力な活性を示します。 | ||
| E4914 | Cabozantinib hydrochloride | Cabozantinib hydrochloride(XL184, BMS-907351 hydrochloride) is a potent small-molecule kinase inhibitor of c-MET and VEGFR2 with an IC50 of 1.3 nM, 0.035 nM respectively. It also inhibits RET, KIT, AXL, Tie2 and FLT3 with an IC50's of 5.2 nM, 4.6 nM, 7 nM, 14.3 nM, 11.3nM respectively. It can be promising agent for inhibiting tumor angiogenesis and metastasis in cancers with dysregulated MET and VEGFR signaling. | ||
| S0439 | UNC2541 | UNC2541 is a potent and specific inhibitor of Mer tyrosine kinase (MerTK) that binds in the MerTK ATP pocket with IC50 of 4.4 nM. UNC2541 inhibits phosphorylated MerTK (pMerTK) with EC50 of 510 nM. | ||
| D4038 | 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。 |
|
|
| 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。 |
|
|
| 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. |
|
|
| 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. |
|
|
| 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). | ||
| 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. |
|
|
| S1497 | Pralatrexate | Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis. |
|
|
| S7342 | UNC2250 | UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3. |
|
|
| S8696 | 2-D08 | 2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. | ||
| 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. |
|
|
| S8619 | NCT-503 | NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with the IC50 value of 2.5 μM. It is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. |
|
|
| S7669 | NPS-1034 | NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7545 | G-749 | G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, showing lower potency against other tyrosine kinases. | ||
| E5942New | UNC9426 | UNC9426 (compound 12) is a potent and orally bioavailable inhibitor of TYRO3 with an IC50 of 2.1 nM. It reduces platelet aggregation without prolonging bleeding time and effectively suppresses TYRO3-mediated signalling pathways in tumor cells and macrophages. | ||
| 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. | ||
| E7462New | Merestinib dihydrochloride | メレスチニブ二塩酸塩（LY2801653二塩酸塩）は、強力で経口投与可能なc - Met阻害剤（Ki = 2 nM）で、抗腫瘍活性を有しています。メレスチニブ二塩酸塩は、MST1R（IC50 = 11 nM）、FLT3（IC50 = 7 nM）、AXL（IC50 = 2 nM）、MERTK（IC50 = 10 nM）、TEK（IC50 = 63 nM）、ROS1、DDR1/2（IC50 = 0.1/7 nM）およびMKNK1/2（IC50 = 7 nM）に対しても強力な活性を示します。 | ||
| E4914 | Cabozantinib hydrochloride | Cabozantinib hydrochloride(XL184, BMS-907351 hydrochloride) is a potent small-molecule kinase inhibitor of c-MET and VEGFR2 with an IC50 of 1.3 nM, 0.035 nM respectively. It also inhibits RET, KIT, AXL, Tie2 and FLT3 with an IC50's of 5.2 nM, 4.6 nM, 7 nM, 14.3 nM, 11.3nM respectively. It can be promising agent for inhibiting tumor angiogenesis and metastasis in cancers with dysregulated MET and VEGFR signaling. | ||
| S0439 | UNC2541 | UNC2541 is a potent and specific inhibitor of Mer tyrosine kinase (MerTK) that binds in the MerTK ATP pocket with IC50 of 4.4 nM. UNC2541 inhibits phosphorylated MerTK (pMerTK) with EC50 of 510 nM. | ||
| D4038 | 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. | ||
| A2851 | Emactuzumab (Anti-CSF1R / M-CSFR / CD115) | Emactuzumab (Anti-CSF1R / M-CSFR / CD115) is a humanized monoclonal antibody directed against the tyrosine kinase receptor colony stimulating factor 1 receptor (CSF1R, CSF-1R, CD115), also known as macrophage colony-stimulating factor receptor (M-CSFR), with potential antineoplastic and immunomodulating activities MW : 146.94 KD. | ||
| 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. | ||
| E5942New | UNC9426 | UNC9426 (compound 12) is a potent and orally bioavailable inhibitor of TYRO3 with an IC50 of 2.1 nM. It reduces platelet aggregation without prolonging bleeding time and effectively suppresses TYRO3-mediated signalling pathways in tumor cells and macrophages. | ||
| E7462New | Merestinib dihydrochloride | メレスチニブ二塩酸塩（LY2801653二塩酸塩）は、強力で経口投与可能なc - Met阻害剤（Ki = 2 nM）で、抗腫瘍活性を有しています。メレスチニブ二塩酸塩は、MST1R（IC50 = 11 nM）、FLT3（IC50 = 7 nM）、AXL（IC50 = 2 nM）、MERTK（IC50 = 10 nM）、TEK（IC50 = 63 nM）、ROS1、DDR1/2（IC50 = 0.1/7 nM）およびMKNK1/2（IC50 = 7 nM）に対しても強力な活性を示します。 |
TAM receptors (Tyro-3,Axl,and Mertk)シグナル伝達経路
納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間