ASTX660

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ASTX660 是一种新型强效 IAP 拮抗剂，靶向 cIAP1/2 和 XIAP 的 BIR3 结构域，IC50 为 12 nM 且 <40 nM。

ASTX660 is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM; potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cell; induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.Blood Cancer Phase 2 Clinical(In Vitro):ASTX660 is an orally bioavailable dual antagonist of cIAP and XIAP, currently being investigated in a single-agent Phase 1/2 clinical trial in patients with advanced solid tumors and lymphomas. Twenty-one triple-negative breast cancer (TNBC) cell lines are treated with ASTX660 in vitro and it is found that 43% are sensitive to ASTX660.(In Vivo):In HCC1806 xenografts in mice, ASTX660 (daily oral treatment) causes moderate tumor growth inhibition but not regression.

Tolinapant is an orally bioavailable dual antagonist of cIAP and XIAP, currently being investigated in a single-agent Phase 1/2 clinical trial in patients with advanced solid tumors and lymphomas. Twenty-one triple-negative breast cancer (TNBC) cell lines are treated with Tolinapant in vitro and it is found that 43% are sensitive to Tolinapant.

In HCC1806 xenografts in mice, Tolinapant (daily oral treatment) causes moderate tumor growth inhibition but not regression.

ASTX 660 | ASTX-660

Apoptosis

IAP

IAP

Cancer

Blood cancer

1799328-86-1

539.696

C30H42FN5O3

>98% (HPLC)

DMSO : ≥ 50 mg/mL 92.65 mM

CC1CN(C(CN1)CN2CCOCC2C)CC(=O)N3CC(C4=C3C=C(C(=N4)CO)CC5=CC=C(C=C5)F)(C)C

1-(6-(4-fluorobenzyl)-5-(hydroxymethyl)-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