H3B-6527


CAS No. : 1702259-66-2

1702259-66-2
Price and Availability of CAS No. : 1702259-66-2
Size Price Stock
1mg $80 In-stock
5mg $210 In-stock
10mg $350 In-stock
25mg $750 In-stock
50mg $1400 In-stock
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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)
Introduction of 1702259-66-2 :

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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