XIAP/cIAP1 antagonist-1


CAS No. : 1403898-55-4

1403898-55-4
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Cat. No. : HY-102051
M.Wt: 509.66
Formula: C29H40FN5O2
Purity: >98 %
Solubility: 10 mM in DMSO
Introduction of 1403898-55-4 :

XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo[1]. In Vitro: XIAP/cIAP1 antagonist-1 (compound 26) shows antiproliferation activity in MDA-MB-231 cells witn an IC50 value of 4.4 nM[1]. In Vivo: XIAP/cIAP1 antagonist-1 (compound 26) (7.5, 15, 30 mg/kg; p.o.; daily for 24 days) inhibits the tumor growth in dose-dependent manner[1].
XIAP/cIAP1 antagonist-1 (1 mg/kg for i.v.; 5, 30 mg/kg for p.o.) shows oral bioavailability (F=22%) at 5 mg/kg[1].
Pharmacokinetic Parameters of XIAP/cIAP1 antagonist-1 in Balb/c SCID mice[1].
dose (mg/kg) route Tmax (h) Cmax (µg/mL) CLp (mL/min/kg) Vss (L/kg) half life (h) AUC (µg·h/mL) F (%)
1 IV 40.9 6.4 3.0 0.41
5 PO 2 0.12 1.8 0.45 22
30 PO 1 1.7 12.1

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