• 阻害剤の選択性比較
  • 溶解度
カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
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
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
S2703 GSK1838705A <1 mg/mL 107 mg/mL <1 mg/mL
S8700 TP0427736 HCl <1 mg/mL 67 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
S8230 Ensartinib (X-396) <1 mg/mL 100 mg/mL 100 mg/mL
製品コード 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

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.


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.


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.


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.



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.


TP0427736 HCl

TP0427736 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.



AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency.



ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.


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.



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).


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.


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). "



ML347 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.


Ensartinib (X-396)

Ensartinib (X-396) is a novel, potent and specific ALK TKI with the IC50 less than 4 nM in Ambit assays.

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