CAS No. : 1621862-70-1

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Cat. No. : HY-100021
M.Wt: 518.57
Formula: C27H33F3N4O3
Purity: >98 %
Storage: at 20℃ 2 years
Solubility: DMSO : ≥ 50 mg/mL (96.42 mM)
Introduction of 1621862-70-1 :

CPI-1205, a highly potent and selective EZH2 inhibitor (biochemical IC50=2 nM, cellular EC50=32 nM). IC50 & Target: IC50: 2 nM (EZH2)[1] In Vitro: When tested within an in vitro hERG binding assay at concentration ranges of 45 nM to 100 μM, CPI-1205 shows an IC50 of 21.3 μM. CPI-1205 demonstrates modest selectivity (EZH1 IC50 of 52±11 nM) when tested against enhancer of zeste homologue 1 (EZH1), a methyltransferase highly related to EZH2. CPI-1205 achieves unbound exposures well above their respective cellular potencies; however, only the unbound exposure for CPI-1205 remains well above the cellular EC50 up to 4 h[1]. In Vivo: CPI-1205 is dosed at 160 mg/kg orally twice daily (po BID) for 25 days in tumor bearing female CB-17 SCID mice. Upon treatment of tumor-bearing CB-17 SCID mice with CPI-1205, tumor regression is observed within 2 weeks. By the end of day 25, significant tumor growth inhibition is recorded (>97% TGI relative to vehicle). CPI-1205 demonstrates robust antitumor effects in a Karpas-422 xenograft model when dosed at 160 mg/kg BID. CPI-1205 shows excellent oral bioavailability. CPI-1205 exhibits moderate clearance of 2.16 L/h/kg (40% liver blood flow), a half-life of ~1.6 h, similar volume of distribution (1.4 L/kg), and excellent bioavailability (100% F)[1].

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