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| Cat. No. : | HY-102051 |
| M.Wt: | 509.66 |
| Formula: | C29H40FN5O2 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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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