XIAP/cIAP1 antagonist-1

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1403898-55-4

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

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。

生物活性

XIAP/cIAP1 antagonist-1 is a potent and orally activeXIAP/cIAP1antagonist withEC₅₀s of 5.1 nM and 0.32 nM forXIAPandcIAP1, 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 IC₅₀value of 4.4 nM^[1].

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	T_max(h)	C_max(μg/mL)	CL_p(mL/min/kg)	V_ss(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

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.