AT-IAP

Research use only, not for human use.

A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively.

A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively; exhibits MDA-MB-231 cell proliferation inhibition with IC50 of 4.4 nM; decreases basal and TNF-α-induced cIAP-1 expression in CaP cells, switches TNF-α signaling from pro-survival to pro-apoptotic and increases radiation sensitivity of CaP cells in co-culture with THP-1 cells; shows in vivo efficacy in Balb/c scid mice bearing MDA-MB-231 xenografts.

XIAP/cIAP1 antagonist-1 (compound 26) shows antiproliferation activity in MDA-MB-231 cells witn an IC50 value of 4.4 nM.

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.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. Pharmacokinetic Parameters of XIAP/cIAP1 antagonist-1 in Balb/c SCID mice. Animal Model:Balb/c SCID mice bearing MDA-MB-231 xenografts 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 Dosage:Administration:1 mg/kg for i.v.; 5, 30 mg/kg for p.o.Result:Showed oral bioavailability (F=22%).

AT IAP

Apoptosis

IAP

IAP

Cancer

——

1403898-55-4

509.67

C29H40FN5O2

>98% (HPLC)

——

O=C(N1CC(C)(C)C2=NC=C(CC3=CC=C(F)C=C3)C=C21)CN4[C@@H](CN5[C@H](C)COCC5)CN[C@H](C)C4

1-(6-(4-fluorobenzyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)-2-((2R,5R)-5-methyl-2-(((R)-3-methylmorpholino)methyl)piperazin-1-yl)ethan-1-one

(-20℃)

With Ice Pack

≥ 2 years