性能参数

产品名称

POMHEX

规格

5 mg 10 mg 25 mg 50 mg

货号

GOY-Y3323

 含量

>99.00%

CAS

2004714-34-3

别名

N/A

化学名

N/A

分子式

C17H30NO9P

分子量

分子量 423.4

溶解度

DMSO : 100 mg/mL (236.18 mM; Need ultrasonic)

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX, is a potent, ENO2-specific inhibitor of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis inhibitor[1].

POMHEX (78 nM, 8h) minimally impacts ENO1-WT glioma cells but profoundly affected ENO1-deleted cells[1].POMHEX (0-720 nM) selectively induces energy stress, inhibits proliferation and triggers apoptosis in ENO1-deleted glioma cells[1].

POMHEX (i.v., ip) injections are consistently tolerated without haemolytic anaemia at doses of up to 10 mg per kg (body weight) per day. POMHEX (i.v., 35 mg/kg) results in lethargy that prompted veterinarians to perform euthanasia[1].POMHEX is rapidly hydrolysed to HemiPOMHEX in mouse plasma ex vivo, with a half-lifeof approximately 30 s, the half-life in human blood ex vivo was about 9min[1].

[1]. Yu-Hsi Lin, et al. An enolase inhibitor for the targeted treatment of ENO1-deleted cancers. Nat Metab. 2020 Nov 23.

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