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BION106 is a PROTAC degrader targeting dihydrofolate reductase-thymidylate synthase (DHFR-TS). It exhibits potent antimalarial activity with a Ki value of 2.68 nM against Plasmodium falciparum and a toxicity of 0.2 μM. For mammalian cells, its Ki value exceeds 100 μM and the toxicity is 44.2 μM. BION106 is suitable for antimalarial research.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | BION106 is a PROTAC degrader targeting dihydrofolate reductase-thymidylate synthase (DHFR-TS). It exhibits potent antimalarial activity with a Ki value of 2.68 nM against Plasmodium falciparum and a toxicity of 0.2 μM. For mammalian cells, its Ki value exceeds 100 μM and the toxicity is 44.2 μM. BION106 is suitable for antimalarial research. |
| In vitro | BION106, when used at 10 μM for 30 to 240 minutes, rapidly and effectively degrades the dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum, indicating its ability to quickly form an effective ternary complex to initiate the degradation process. Additionally, BION106 at concentrations ranging from 0.4 to 50 μM over 4 hours significantly reduces the enzyme levels in a concentration-dependent manner. |
| Molecular Weight | 1133.13 |
| Formula | C57H69Cl2F2N9O9 |
| Cas No. | 3077918-44-3 |
| Smiles | C(#N)[C@]1([C@H]([C@H](C(NC2=C(OC)C=C(C(NCCOCCOCCOCCNC(CCC3=C(OCCCOC=4C(CC)=NC(N)=NC4N)C=CC=C3)=O)=O)C=C2)=O)N[C@H]1CC(C)(C)C)C5=C(F)C(Cl)=CC=C5)C6=C(F)C=C(Cl)C=C6 |
| 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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