T-3256336

Research use only, not for human use.

A potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively.

A potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively; dose dependently antagonizes XIAP and promotes the activities of caspase-3 with EC50 of 1.3 uM in cell-free assays, induces the rapid proteasomal degradation of cIAP-1 and activates TNF-α-dependent extrinsic apoptosis signaling in cultured cells; induces cIAP-1 degradation, TNF-α production and caspase activation in cancer xenograft models.

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Animal Model:Female BALB/cAJcl mice (MDA-MB-231-Luc xenograft)Dosage:30, 100 mg/kg Administration:P.o.Result:Stimulated caspase-3/7 activity in a dose-dependent manner, induced tumor regression in a dose-dependent manner with a percent tumor growth inhibition (T/C) of 53% and 62% at 30 mg/kg and 100 mg/kg, respectively.

T3256336 | T 3256336

Apoptosis

IAP

IAP

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1266227-69-3

605.728

C31H45F2N5O5

>98% (HPLC)

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O=C([C@H]1N(C([C@H](C2CCC(F)(F)CC2)NC([C@H](C)NC)=O)=O)C[C@](C[C@@H](OCC)C3)([H])N3C1)N[C@@H]4CCOC5=C4C=CC=C5

Pyrrolo[1,2-a]pyrazine-3-carboxamide, 2-[(2S)-2-(4,4-difluorocyclohexyl)-2-[[(2S)-2-(methylamino)-1-oxopropyl]amino]acetyl]-N-[(4R)-3,4-dihydro-2H-1-benzopyran-4-yl]-7-ethoxyoctahydro-, (3S,7R,8aR)-

(-20℃)

With Ice Pack

≥ 2 years