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PTC299

Chemical Structure : PTC299

CAS No.: 1256565-36-2

PTC299 (Emvododstat;PTC-299;PTC 299)

Catalog No.: PC-35755Not For Human Use, Lab Use Only.

Emvododstat (PTC-299) is a novel potent inhibitor of dihydroorotate dehydrogenase (DHODH), inhibits hypoxia-induced VEGFA protein production in HeLa cells with IC50 of 1.64 nM.

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Biological Activity

Emvododstat (PTC-299) is a novel potent inhibitor of dihydroorotate dehydrogenase (DHODH), inhibits hypoxia-induced VEGFA protein production in HeLa cells with IC50 of 1.64 nM.
PTC299 inhibited DHODH activity more potently than teriflunomide and with potency similar to that of brequinar.
PTC299 demonstrates broad and potent activity against hematological cancer cells in preclinical models, inhibits AML patient-derived cells with IC50 of 2-60 nM.
PTC299 demonstrates advantages over previously reported DHODH inhibitors, including greater potency, good oral bioavailability and lack of off-target kinase inhibition and myelosuppression.

Physicochemical Properties

M.Wt 467.346
Formula C25H20Cl2N2O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

100 mM in DMSO (46.7 mg/mL, ultrasonic needed)

Chemical Name/SMILES

4-chlorophenyl (S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indole-2-carboxylate

References

1. Cao L, et al. Mol Cancer Ther. 2018 Oct 23. pii: molcanther.0863.2018.

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