ALK
Signaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S1068 | Crizotinib (PF-02341066) | <1 mg/mL | 9 mg/mL | <1 mg/mL |
| S1108 | TAE684 (NVP-TAE684) | <1 mg/mL | 3 mg/mL | <1 mg/mL |
| S2762 | Alectinib (CH5424802) | <1 mg/mL | 0.5 mg/mL | <1 mg/mL |
| S7083 | Ceritinib (LDK378) | <1 mg/mL | 20 mg/mL | 3 mg/mL |
| S7000 | AP26113-analog (ALK-IN-1) | <1 mg/mL | 45 mg/mL | 106 mg/mL |
| S8700 | TP0427736 HCl | <1 mg/mL | 67 mg/mL | <1 mg/mL |
| S5232 | Alectinib hydrochloride | <1 mg/mL | 2 mg/mL | <1 mg/mL |
| S2703 | GSK1838705A | <1 mg/mL | 107 mg/mL | <1 mg/mL |
| S7106 | AZD3463 | <1 mg/mL | 24 mg/mL | <1 mg/mL |
| S8054 | ASP3026 | <1 mg/mL | 14 mg/mL | <1 mg/mL |
| S7998 | Entrectinib (RXDX-101) | <1 mg/mL | 100 mg/mL | 75 mg/mL |
| S8583 | TPX-0005 | <1 mg/mL | 70 mg/mL | 10 mg/mL |
| S8229 | Brigatinib (AP26113) | <1 mg/mL | 1 mg/mL | 43 mg/mL |
| S8511 | Belizatinib (TSR-011) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S7148 | ML347 | <1 mg/mL | 10 mg/mL | <1 mg/mL |
| S7536 | Lorlatinib (PF-6463922) | <1 mg/mL | 81 mg/mL | 30 mg/mL |
| S8230 | Ensartinib (X-396) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
- ALK Inhibitors (17)
- New ALK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1068 |
Crizotinib (PF-02341066)Crizotinib (PF-02341066) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. |
(c) Western blot analyses of p-Akt (Ser473) and p-S6RP (Ser235 and Ser236) in two RCT-E565 transplanted tumors treated with vehicle or PF02341066. Samples were isolated 4 h after the last dose from mice treated with PF02341066 for 3 d. (d) Responses of RCT-E565 transplanted tumors in athymic mice to PF02341066 or vehicle. Data are means ±s.e.m. (each group, n = 6). *P < 0.005, **P < 0.001 (Student,s t test). |
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| S1108 |
TAE684 (NVP-TAE684)TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR. |
(A) H3122 xenografts harboring the EML4-ALK translocation were treated with control vehicle or the ALK inhibitor, TAE-684, for 2 days; the tumors were excised and lysates were prepared. The TIMM results for the control and treated animals are shown. (B) H3122 cells were treated in the presence or absence of TAE-684 (100 nM) for 6 hours in the presence or absence of the indicated ligands [EGF (50 ng/mL), IGF1 (50 ng/mL), and HGF (50 ng/mL)]. Extracts were probed with the indicated antibodies. |
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| S2762 |
Alectinib (CH5424802)Alectinib (CH5424802) 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. |
Immunoblot analysis of full-length DCTN1-ALK proteins. An expression vector encoding DCTN1-ALK cDNA was introduced into H1299 lung cancer cells, which do not express endogenous ALK. The transfectants were then exposed to crizotinib and alectinib. Levels of phosphorylation at tyrosine 1604 were determined 24 hours after treatment with 0, 0.2, 1.0, or 5.0 μM of each drug.
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| S7083 |
Ceritinib (LDK378)Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3. |
Quantitation of crystal violet uptake by ORF-expressing cells exposed to crizotinib (CRZ) or ceritinib (CER) normalized to Lac Z. Mean and SE are shown for six (CRZ) or four (CER) independent experiments of three replicates each.
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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. |
Several ALK inhibitors effectively inhibit the growth of CD74–ROS1–addicted Ba/F3 cells. A, Ba/F3 cells expressing CD74–ROS1 (clone #6) were seeded in 96-well plates and treated with the indicated concentration of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 72 hours. Cell viability was analyzed using the CellTiter-Glo Assay. B, IC50 values (nmol/L) of Ba/F3 cell lines expressing CD74–ROS1 (clone #6) against various ALK inhibitors are shown. Average IC50 values against crizotinib, ceritinib, or AP26113 were calculated from the three independent experiments. IC50 values against ASP3026 and alectinib were calculated from the single experiment. C, inhibition of phospho-ROS1 by various ALK inhibitors in Ba/F3 models. CD74–ROS1–expressing Ba/F3 cells were exposed to increasing concentrations of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 3 hours. Cell lysates were immunoblotted to detect the indicated proteins. |
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| S8700New |
TP0427736 HClTP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. |
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| S5232New |
Alectinib hydrochlorideAlectinib is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase. |
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| S2703 |
GSK1838705AGSK1838705A 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. |
Protective effect of IGF1 on Sorafenib or VK1-mediated actin cytoskeleton redistribution in HCC cells. PLC/PRF/5 and HLF cells were stained with DyLight 554 Phalloidin after treatment with 1 μM Sorafenib, 12 μM VK1 or 1 μM GSK1838705A (GSK) for 24 h alone or in combination with 40 ng/ml IGF1. Scale bar: 100 μm.
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| S7106 |
AZD3463AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. |
(E) Immunoblot analysis of lysates of A4573 and TC32 cells following exposure to media only (Control, C); ST/V and V/ST with (+) or without (-) 20 nM AZD3463 using antibodies against ALK, IGF-1R, STAT3 (Y705), p-STAT3, AKT, p-AKT (S473), MAPK, p-MAPK (p42/44). |
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| S8054 |
ASP3026ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1. |
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| S7998 |
Entrectinib (RXDX-101)Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2. |
(A) We transfected the EGFP/Eluc gene into KM12SM cells to establish KM12SM/Eluc cells. KM12SM/Eluc cells were inoculated into the brain of SCID mice. The mice were treated daily with or without entrectinib (15 mg/kg) for 37 days until the bioluminescence increased. Mean ± SE of total flux are shown in the lower panel. Then, the entrectinib-treated brain tumor was harvested at the point indicated by the orange triangle and cultured in vitro. The expanded tumor cells were named KM12SM-ER. (B) The sensitivity of KM12SM-ER and KM12SM cells to entrectinib was determined through cell viability assays, using a CCK-8 kit. The data (mean ± standard deviation [SD] of triplicate cultures) shown are representative of three independent experiments with similar results. (C) Tumor cells were treated with entrectinib (10 nmol/L) for 4 h or c-PARP for 48 h, and harvested lysates were assessed by western blotting. Data shown are representative of three independent experiments with similar results.
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| S8583 |
TPX-0005TPX-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). |
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| S8229 |
Brigatinib (AP26113)Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy. |
Immunoblotting analysis of H3122 and H3122-CER cells showing that brigatinib did not inhibit EGFR phosphorylation (p-EGFR). Total EGFR (t-EGFR) is also shown. Actin was used as a loading control. The cells were treated with brigatinib for 2 hours.
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| 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). " |
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| S7148 |
ML347ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM. |
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| S7536 |
Lorlatinib (PF-6463922)PF-06463922 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. Phase 1. |
Sub-G1 and cell cycle phase distribution of NBLW and NBLW-R cells treated for 24 hours with DMSO, 1× or 10× the respective GI 50 concentrations of PF-06463922.
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| S8230 |
Ensartinib (X-396)Ensartinib (X-396) is a novel, potent and specific ALK TKI with the IC50 less than 4 nM in Ambit assays. |
