Size | Price | Stock |
---|---|---|
1mg | $40 | In-stock |
5mg | $120 | In-stock |
10mg | $220 | In-stock |
25mg | $420 | In-stock |
50mg | $670 | In-stock |
100 mg | Get quote | |
200 mg | Get quote | |
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Cat. No. : | HY-100517 |
M.Wt: | 333.38 |
Formula: | C20H19N3O2 |
Purity: | >98 % |
Solubility: | DMSO : 100 mg/mL (299.96 mM; ultrasonic and warming and heat to 60°C) |
TP-472 is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7[1][2]. TP-472 induces apoptosis of melanoma cells[3].
IC50 & Target:Kd: 33 nM (BRD9)[1]
In Vitro:TP-472 (1 µM, 3 µM; 24-216 hours) yields concentration-dependent growth defects in ESCs[2].
TP-472 (0.1-10 μM; 24 h) effectively inhibits the growth of both the BRAF mutant melanoma cell lines at 5 and 10 µM concentrations[3].
TP-472 (for 2 weeks) also strongly inhibits the long-term survival of multiple melanoma cell lines (M14, SKMEL-28, A375, and A2058) at concentrations of 5 and 10 µM[3].
TP-472 (5-10 μM; 24 h) treatment downregulates genes encoding various extracellular matrix (ECM) proteins, including integrins, collagens, and fibronectins in A375 cells[3].
TP-472 (0.1-10 μM; 24 h) results in the upregulation of pro-apoptotic genes (BAX, MDM2, CDKN1A) in A375 cells[3].
In Vivo:TP-472 (20 mg/kg; i.p.; three times a week; for 5 weeks) significantly inhibits the subcutaneous tumor growth in melanoma xenograft mouse model[3].
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