[CAS NO. 2004714-34-3] POMHEX
PRODUCTS SPECIFICATIONS [2004714-34-3]
DESCRIPTION [2004714-34-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 423.40 |
| Molecular Formula | C17H30NO9P |
| SMILES | O=P(OCOC(C(C)(C)C)=O)(OCOC(C(C)(C)C)=O)C1C(N(O)CCC1)=O |
Summary
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] .
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [1]
| Cell Line: | ENO1-deleted (D423, red), ENO1-isogenically rescued (D423 ENO1, blue) and ENO1-WT (LN319, grey) cells. |
| Concentration: | 78 nM. |
| Incubation Time: | 8 h. |
| Result: | Down-regulated cell density. |
In Vivo
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-life of approximately 30 s, the half-life in human blood ex vivo was about 9min
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 236.18 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3618 mL | 11.8092 mL | 23.6183 mL |
| 5 mM | 0.4724 mL | 2.3618 mL | 4.7237 mL |
| 10 mM | 0.2362 mL | 1.1809 mL | 2.3618 mL |