Size | Price | Stock |
---|---|---|
1mg | $80 | In-stock |
5mg | $210 | In-stock |
10mg | $350 | In-stock |
25mg | $750 | In-stock |
50mg | $1400 | In-stock |
100 mg | Get quote | |
200 mg | Get quote | |
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Cat. No. : | HY-100491 |
M.Wt: | 629.54 |
Formula: | C29H34Cl2N8O4 |
Purity: | >98 % |
Solubility: | DMSO : 2.5 mg/mL (3.97 mM; Need ultrasonic) |
H3B-6527 is an orally active, highly selective and covalent FGFR4 inhibitor with an IC50 of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC50s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity[1].
In Vitro: H3B-6527 inhibits TAOK2, JNK2, and CSF1R with IC50s of 690 nM, >10000 nM, and >10000 nM, respectively[1].
H3B-6527 (10-10000 nM; 72 hours) results in a GI50 value of 25 nM[1].
H3B-6527 (10-10000 nM; 72 hours) leads cell death in HCC cell lines[1].
H3B-6527 (0.1-1000 nM; 1 hour) decreases the levels of pERK1/2 in a dose-dependent manner with maximal inhibition occurring at 100 nM[1].
H3B-6527 (1-1000 nM; 24 hours) causes a robust increase in CYP7A1 transcripts[1].
In Vivo: H3B-6527 (10-300 mg/kg; orally; twice-daily; for 15 days) significantly inhibits tumor growth at the 300 and 100 mg/kg and does not inhibit tumor growth at 30 and 10 mg/kg[1].
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