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ALK
ALK製品
- All (32)
- ALK阻害剤 (29)
- ALK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 |
|---|---|---|---|---|
| S1068 | Crizotinib | Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. |
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| S7083 | Ceritinib | Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3. |
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| S1108 | TAE684 (NVP-TAE684) | TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM of 3 nM, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis. |
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| S2762 | Alectinib | Alectinib is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429. |
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| S5190 | Crizotinib hydrochloride | Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. | ||
| S7536 | Lorlatinib (PF-6463922) | Lorlatinib (PF-6463922) is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. PF-06463922 induces apoptosis. Phase 1. |
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| S7998 | Entrectinib | Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2. |
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|
| S8229 | Brigatinib | Brigatinib is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy. |
|
|
| S5232 | Alectinib (CH5424802) hydrochloride | Alectinib (AF802, CH5424802, RO5424802, RG-7853) is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. | ||
| S2703 | GSK1838705A | GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases. |
|
|
| S4967 | Ceritinib dihydrochloride | Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitomor activity. | ||
| S8583 | Repotrectinib (TPX-0005) | Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM). | ||
| S7106 | AZD3463 | AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy. |
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| S7000 | AP26113-analog (ALK-IN-1) | AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR. |
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|
| S8054 | ASP3026 | ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1. | ||
| S2934 | Ensartinib dihydrochloride | Ensartinib dihydrochloride is a potent new-generation ALK inhibitor with high activity against a broad range of known crizotinib-resistant ALK mutations and CNS metastases. It potently inhibits both wild-type ALK and ALK variants (F1174, C1156Y, L1196M, S1206R, T1151, and G1202R mutants) with in vitro IC50s of <4 nM. | ||
| S6513 | HG-14-10-04 | HG-14-10-04 is an inhibitor of ALK. | ||
| S6505 | X-376 | X-376 is an ALK inhibitor and potentially useful in non-small cell lung cancer. | ||
| E2836 | ALK inhibitor 1 | ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM). | ||
| E1846New | TL13-112 | TL13-112 is a degrader of anaplastic lymphoma kinase (ALK) with an IC50 of 0.60 nM. It demonstrates anti-proliferative activity in non-small-cell lung cancer (NSCLC) and anaplastic large cell lymphoma (ALCL) cell lines. | ||
| E1508New | APG-2449 | APG-2449 is an orally active inhibitor of ALK/ROS1/FAK. APG-2449 exerts potent and durable antitumor activity in human non-small-cell lung cancer (NSCLC) and ovarian tumor models. | ||
| E1865New | Envonalkib | Envonalkib(TQ-B3139, CT-71, Formula 1) is a potent and orally active inhibitor of ALK, that exhibits IC50 values of 1.96 nM, 35.1 nM, and 61.3 nM for wild-type and mutated L1196M and G1269S-ALK. Envonalkib is also used in the research of non-small cell lung cancer. | ||
| E1961New | NVL-655 | NVL-655 is a selective inhibitor of anaplastic lymphoma kinase (ALK), with potential antineoplastic activity in the Ba/F3 xenograft model. It also exhibits significant inhibitory activity against ROS1, LTK, PYK2, TRKB, and FAK, with an IC50 ≤10-fold ALK and demonstrates high potency against specific ALK mutations, with an IC50 of <0.73 nM, 7 nM, 3 nM, 3 nM for G1202R, G1202R/L1196M, G1202R/G1269A and G1202R/L1198F respectively. | ||
| E1783New | Conteltinib(CT-707) | Conteltinib(CT-707) is a potent multikinase inhibitor of ALK, FAK,Pyk2, showing promising anti-tumor activities. Conteltinib exhibits significant inhibitory effects on FAK with an IC50 value of 1.6 nM in vitro kinase assay. | ||
| A2621 | Anti-ACVR1 / ALK-2 (DS-6016a) | Anti-ACVR1 / ALK-2 (DS-6016a) monoclonal antibody targeting ALK-2. It can be used in the treatment of fibrodysplasia ossificans progressiva (FOP). MW :145.56. | ||
| E1565New | Iruplinalkib | Iruplinalkib (WX-0593) is a highly selective oral inhibitor of ALK and ROS1 tyrosine kinase. It exhibits potent and promising antitumor activity in advanced non-small cell lung cancer (NSCLC) with ALK or ROS1 rearrangement. | ||
| S0072 | MS4078 | MS4078 is an inhibitor and PROTAC (degrader) of ALK. MS4078 reduces the NPM-ALK protein levels in SU-DHL-1 cells and the EML4-ALK protein levels in NCI-H2228 cells with DC50 of 11 nM and 59 nM, respectively. MS4078 induces ALK protein degradation via cereblon and proteasome dependent mechanism and potently inhibits proliferation of SU-DHL-1 cells with IC50 of 33 nM. | ||
| S8511 | Belizatinib (TSR-011) | "Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). " | ||
| E1507 | Zilurgisertib fumarate | Zilurgisertib fumarate(INCB-000928 fumarate, NBU-928 fumarate) is a selective ALK 2 inhibitor.It is under development for the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva. | ||
| E1732 | Itacnosertib (TP-0184) | Itacnosertib (TP-0184) is a small-molecule inhibitor of the BMP type 1 receptor ALK2 (also known as ACVR1). Itacnosertib reduces hepcidin induction and elevated serum iron levels in turpentine and lung cancer mouse models of ACD. | ||
| A2594 | Ascrinvacumab (Anti-ACVRL1 / ALK-1) | Ascrinvacumab (Anti-ACVRL1 / ALK-1) is a human IgG2 monoclonal antibody targeting ALK-1. It can be used for the treatment of hepatocellular carcinoma (HCC), in patients with advanced solid tumors. It also demonstrates its use in antiangiogenic therapy. MW : 150 KD. | ||
| E0958 | ZX-29 | ZX-29 is a potent and selective ALK inhibitor with an IC50s of 2.1, 1.3 and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. | ||
| S1068 | Crizotinib | Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. |
|
|
| S7083 | Ceritinib | Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3. |
|
|
| S1108 | TAE684 (NVP-TAE684) | TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM of 3 nM, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis. |
|
|
| S2762 | Alectinib | Alectinib is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429. |
|
|
| S5190 | Crizotinib hydrochloride | Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. | ||
| S7536 | Lorlatinib (PF-6463922) | Lorlatinib (PF-6463922) is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. PF-06463922 induces apoptosis. Phase 1. |
|
|
| S7998 | Entrectinib | Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2. |
|
|
| S8229 | Brigatinib | Brigatinib is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy. |
|
|
| S5232 | Alectinib (CH5424802) hydrochloride | Alectinib (AF802, CH5424802, RO5424802, RG-7853) is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. | ||
| S2703 | GSK1838705A | GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases. |
|
|
| S4967 | Ceritinib dihydrochloride | Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitomor activity. | ||
| S8583 | Repotrectinib (TPX-0005) | Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM). | ||
| S7106 | AZD3463 | AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy. |
|
|
| S7000 | AP26113-analog (ALK-IN-1) | AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR. |
|
|
| S8054 | ASP3026 | ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1. | ||
| S2934 | Ensartinib dihydrochloride | Ensartinib dihydrochloride is a potent new-generation ALK inhibitor with high activity against a broad range of known crizotinib-resistant ALK mutations and CNS metastases. It potently inhibits both wild-type ALK and ALK variants (F1174, C1156Y, L1196M, S1206R, T1151, and G1202R mutants) with in vitro IC50s of <4 nM. | ||
| S6513 | HG-14-10-04 | HG-14-10-04 is an inhibitor of ALK. | ||
| S6505 | X-376 | X-376 is an ALK inhibitor and potentially useful in non-small cell lung cancer. | ||
| E2836 | ALK inhibitor 1 | ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM). | ||
| E1508New | APG-2449 | APG-2449 is an orally active inhibitor of ALK/ROS1/FAK. APG-2449 exerts potent and durable antitumor activity in human non-small-cell lung cancer (NSCLC) and ovarian tumor models. | ||
| E1865New | Envonalkib | Envonalkib(TQ-B3139, CT-71, Formula 1) is a potent and orally active inhibitor of ALK, that exhibits IC50 values of 1.96 nM, 35.1 nM, and 61.3 nM for wild-type and mutated L1196M and G1269S-ALK. Envonalkib is also used in the research of non-small cell lung cancer. | ||
| E1961New | NVL-655 | NVL-655 is a selective inhibitor of anaplastic lymphoma kinase (ALK), with potential antineoplastic activity in the Ba/F3 xenograft model. It also exhibits significant inhibitory activity against ROS1, LTK, PYK2, TRKB, and FAK, with an IC50 ≤10-fold ALK and demonstrates high potency against specific ALK mutations, with an IC50 of <0.73 nM, 7 nM, 3 nM, 3 nM for G1202R, G1202R/L1196M, G1202R/G1269A and G1202R/L1198F respectively. | ||
| E1783New | Conteltinib(CT-707) | Conteltinib(CT-707) is a potent multikinase inhibitor of ALK, FAK,Pyk2, showing promising anti-tumor activities. Conteltinib exhibits significant inhibitory effects on FAK with an IC50 value of 1.6 nM in vitro kinase assay. | ||
| E1565New | Iruplinalkib | Iruplinalkib (WX-0593) is a highly selective oral inhibitor of ALK and ROS1 tyrosine kinase. It exhibits potent and promising antitumor activity in advanced non-small cell lung cancer (NSCLC) with ALK or ROS1 rearrangement. | ||
| S0072 | MS4078 | MS4078 is an inhibitor and PROTAC (degrader) of ALK. MS4078 reduces the NPM-ALK protein levels in SU-DHL-1 cells and the EML4-ALK protein levels in NCI-H2228 cells with DC50 of 11 nM and 59 nM, respectively. MS4078 induces ALK protein degradation via cereblon and proteasome dependent mechanism and potently inhibits proliferation of SU-DHL-1 cells with IC50 of 33 nM. | ||
| S8511 | Belizatinib (TSR-011) | "Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). " | ||
| E1507 | Zilurgisertib fumarate | Zilurgisertib fumarate(INCB-000928 fumarate, NBU-928 fumarate) is a selective ALK 2 inhibitor.It is under development for the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva. | ||
| E1732 | Itacnosertib (TP-0184) | Itacnosertib (TP-0184) is a small-molecule inhibitor of the BMP type 1 receptor ALK2 (also known as ACVR1). Itacnosertib reduces hepcidin induction and elevated serum iron levels in turpentine and lung cancer mouse models of ACD. | ||
| E0958 | ZX-29 | ZX-29 is a potent and selective ALK inhibitor with an IC50s of 2.1, 1.3 and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. | ||
| A2621 | Anti-ACVR1 / ALK-2 (DS-6016a) | Anti-ACVR1 / ALK-2 (DS-6016a) monoclonal antibody targeting ALK-2. It can be used in the treatment of fibrodysplasia ossificans progressiva (FOP). MW :145.56. | ||
| A2594 | Ascrinvacumab (Anti-ACVRL1 / ALK-1) | Ascrinvacumab (Anti-ACVRL1 / ALK-1) is a human IgG2 monoclonal antibody targeting ALK-1. It can be used for the treatment of hepatocellular carcinoma (HCC), in patients with advanced solid tumors. It also demonstrates its use in antiangiogenic therapy. MW : 150 KD. | ||
| E1846New | TL13-112 | TL13-112 is a degrader of anaplastic lymphoma kinase (ALK) with an IC50 of 0.60 nM. It demonstrates anti-proliferative activity in non-small-cell lung cancer (NSCLC) and anaplastic large cell lymphoma (ALCL) cell lines. | ||
| E1508New | APG-2449 | APG-2449 is an orally active inhibitor of ALK/ROS1/FAK. APG-2449 exerts potent and durable antitumor activity in human non-small-cell lung cancer (NSCLC) and ovarian tumor models. | ||
| E1865New | Envonalkib | Envonalkib(TQ-B3139, CT-71, Formula 1) is a potent and orally active inhibitor of ALK, that exhibits IC50 values of 1.96 nM, 35.1 nM, and 61.3 nM for wild-type and mutated L1196M and G1269S-ALK. Envonalkib is also used in the research of non-small cell lung cancer. | ||
| E1961New | NVL-655 | NVL-655 is a selective inhibitor of anaplastic lymphoma kinase (ALK), with potential antineoplastic activity in the Ba/F3 xenograft model. It also exhibits significant inhibitory activity against ROS1, LTK, PYK2, TRKB, and FAK, with an IC50 ≤10-fold ALK and demonstrates high potency against specific ALK mutations, with an IC50 of <0.73 nM, 7 nM, 3 nM, 3 nM for G1202R, G1202R/L1196M, G1202R/G1269A and G1202R/L1198F respectively. | ||
| E1783New | Conteltinib(CT-707) | Conteltinib(CT-707) is a potent multikinase inhibitor of ALK, FAK,Pyk2, showing promising anti-tumor activities. Conteltinib exhibits significant inhibitory effects on FAK with an IC50 value of 1.6 nM in vitro kinase assay. | ||
| E1565New | Iruplinalkib | Iruplinalkib (WX-0593) is a highly selective oral inhibitor of ALK and ROS1 tyrosine kinase. It exhibits potent and promising antitumor activity in advanced non-small cell lung cancer (NSCLC) with ALK or ROS1 rearrangement. |
ALK阻害剤の選択性比較
ALKシグナル伝達経路
Tags: ALK inhibition | ALK cancer | ALK mutation | ALK tumor | ALK inhibitor drugs | ALK activation | ALK targets | ALK inhibitor cancer | ALK assay | ALK phosphorylation | ALK signaling pathway | ALK inhibitor clinical trial | ALK inhibitor review
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