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SNX631 is a potent and highly selective CDK8/19 mediator kinase inhibitor with an IC₅₀ of 10.3 nM in NF-κB-dependent cellular assays. Its activity is 6–10 times higher than that of Senexin B in all assays except DiscoverX active site-dependent competitive binding experiments. SNX631 exerts synergistic effects with lapatinib and trastuzumab in multiple HER2-positive breast cancer cell lines, reversing and preventing resistance to HER2-targeted therapy. The combination of trastuzumab (a HER2 monoclonal antibody) and SNX631 inhibits the phosphorylation of STAT1 and STAT3 at the S727 site and upregulates the expression of the tumor suppressor BTG2 in HER2-positive breast cancer cells. SNX631 partially inhibits the growth of lapatinib-sensitive and -resistant HER2-positive breast cancer xenografts, and its antitumor effect is significantly enhanced when combined with lapatinib, effectively overcoming lapatinib resistance.


| Description | SNX631 is a potent and highly selective CDK8/19 mediator kinase inhibitor with an IC₅₀ of 10.3 nM in NF-κB-dependent cellular assays. Its activity is 6–10 times higher than that of Senexin B in all assays except DiscoverX active site-dependent competitive binding experiments. SNX631 exerts synergistic effects with lapatinib and trastuzumab in multiple HER2-positive breast cancer cell lines, reversing and preventing resistance to HER2-targeted therapy. The combination of trastuzumab (a HER2 monoclonal antibody) and SNX631 inhibits the phosphorylation of STAT1 and STAT3 at the S727 site and upregulates the expression of the tumor suppressor BTG2 in HER2-positive breast cancer cells. SNX631 partially inhibits the growth of lapatinib-sensitive and -resistant HER2-positive breast cancer xenografts, and its antitumor effect is significantly enhanced when combined with lapatinib, effectively overcoming lapatinib resistance. |
| Molecular Weight | 438.55 |
| Formula | C22H26N6O2S |
| Cas No. | 868066-26-6 |
| Smiles | O=C(N)C=1SC2=NC=CC(=C2C1N)N3CCN(C4=CC=C(C=C4)C(=O)N(C)C)CCC3 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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