XIAP/cIAP1 antagonist-1

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XIAP/cIAP1 antagonist-1 

XIAP/cIAP1 antagonist-1 是一种有效的且具有口服活性的 XIAP/cIAP1 拮抗剂，XIAP 和 cIAP1 的 EC50 值分别为 5.1 nM 和 0.32 nM。XIAP/cIAP1 antagonist-1 在体内以剂量依赖方式抑制肿瘤生长。

XIAP/cIAP1 antagonist-1

XIAP/cIAP1 antagonist-1 Chemical Structure

CAS No. : 1403898-55-4

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生物活性

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)

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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

上海金畔生物科技有限公司 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%).

分子量

509.66

Formula

C29H40FN5O2
CAS 号

1403898-55-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Tamanini E, et al. Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP). J Med Chem. 2017; 60(11):4611-4625.

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