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  3. XIAP/cIAP1 antagonist-1

XIAP/cIAP1 antagonist-1 

Cat. No.: HY-102051
Handling Instructions

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.

For research use only. We do not sell to patients.

XIAP/cIAP1 antagonist-1 Chemical Structure

XIAP/cIAP1 antagonist-1 Chemical Structure

CAS No. : 1403898-55-4

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Description

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].

IC50 & Target[1]

XIAP

5.1 nM (IC50)

cIAP1

0.32 nM (IC50)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c SCID mice bearing MDA-MB-231 xenografts[1]
Dosage: 7.5, 15, 30 mg/kg
Administration: PO; daily for 24 days
Result: Inhibited the tumor growth in dose-dependent manner.
Animal Model: Balb/c SCID mice bearing MDA-MB-231 xenografts[1]
Dosage:
Administration: 1 mg/kg for i.v.; 5, 30 mg/kg for p.o.
Result: Showed oral bioavailability (F=22%).
Molecular Weight

509.66

Formula

C29H40FN5O2

CAS No.
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XIAP/cIAP1 antagonist-1
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HY-102051
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