Size | Price | Stock |
---|---|---|
5mg | $72 | In-stock |
10mg | $102 | In-stock |
25mg | $180 | In-stock |
50mg | $288 | In-stock |
100mg | $504 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-100996 |
M.Wt: | 332.31 |
Formula: | C18H12N4O3 |
Purity: | >98 % |
Solubility: | DMSO : ≥ 28 mg/mL (84.26 mM) |
10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC50 of 146 μM. IC50 & Target: IC50: 15.6 μM (Daudi cells), 13.5 μM (HL-60 cells)[1], 146 μM (c-Myc–Max)[2] In Vitro: 10074-G5 inhibits the growth of Daudi Burkitt's lymphoma cells and disruptes c-Myc/Max dimerization. The IC50 values against Daudi and HL-60 cells are 15.6 and 13.5 μM, respectively[1]. 10074-G5 binds the Myc peptide Myc353-437 with a Kd value of 2.8 μM in the region Arg363-Ile381. 10074-G5 binds in a cavity that is created by a kink (Asp379-Ile381) in the N-terminus of an induced helical domain (Leu370–Arg378)[3]. In Vivo: The plasma half-life of 10074-G5 in mice treated with 20 mg/kg i.v. is 37 min, and peak plasma concentration was 58 μM, which is 10-fold higher than peak tumor concentration[1].
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