• 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
S1021 Dasatinib <1 mg/mL 98 mg/mL <1 mg/mL
S1006 Saracatinib (AZD0530) <1 mg/mL 35 mg/mL 31 mg/mL
S1014 Bosutinib (SKI-606) <1 mg/mL 100 mg/mL 2 mg/mL
S2700 KX2-391 <1 mg/mL 86 mg/mL <1 mg/mL
S2202 NVP-BHG712 <1 mg/mL 101 mg/mL 3 mg/mL
S8583 TPX-0005 <1 mg/mL 70 mg/mL 10 mg/mL
S7008 PP2 <1 mg/mL 60 mg/mL 2 mg/mL
S2622 PP121 <1 mg/mL 64 mg/mL 2 mg/mL
S7060 PP1 <1 mg/mL 4 mg/mL <1 mg/mL
S4921 MNS (3,4-Methylenedioxy-β-nitrostyrene) <1 mg/mL 39 mg/mL <1 mg/mL
S7565 WH-4-023 <1 mg/mL 12 mg/mL 6 mg/mL
S7782 Dasatinib Monohydrate <1 mg/mL 21 mg/mL <1 mg/mL
S2391 Quercetin <1 mg/mL 61 mg/mL 10 mg/mL
S7774 SU6656 <1 mg/mL 74 mg/mL <1 mg/mL
S7743 CCT196969 <1 mg/mL 100 mg/mL <1 mg/mL
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Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.


Saracatinib (AZD0530)

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3.


Bosutinib (SKI-606)

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively.



KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.



NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.



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).



PP2, a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.



PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.



PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.


MNS (3,4-Methylenedioxy-β-nitrostyrene)

MNS is a tyrosine kinase inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.



WH-4-023 is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.


Dasatinib Monohydrate

Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.



Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Phase 4.



SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.



CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.

Tags: Src activation | Src kinase family | Src family kinases | Src activity | Src cancer | Src tyrosine kinase | Src pathway | Src phosphorylation | Src inhibition | Src kinase pathway | Src kinase assay | Src inhibitors cancer | Src inhibitor clinical trials | Src inhibitor review