PTC299( PTC-299 | PTC 299 )

Catalog No. M11050 CAS No. 1256565-36-2

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PTC299
Note

Research use only, not for human use.
Brief Description

PTC299 (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.
Description

PTC299 (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; inhibited DHODH activity more potently than teriflunomide and with potency similar to that of brequinar, demonstrates broad and potent activity against hematological cancer cells in preclinical models, inhibits AML patient-derived cells with IC50 of 2-60 nM; demonstrates advantages over previously reported DHODH inhibitors, including greater potency, good oral bioavailability and lack of off-target kinase inhibition and myelosuppression.Breast Cancer Phase 1 Clinical.
In Vitro

PTC299 inhibits hypoxia-induced VEGFA protein production in HeLa cells with an EC50 of 1.64 ± 0.83 nM.PTC299 is the most potent inhibitor with an IC50 of about 1 nM, over 10 to 1000-fold more potent than Brequinar, Vidofludimus or A 77-1726 in leukemia cells.
In Vivo

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Synonyms

PTC-299 | PTC 299
Pathway

Others
Target

Other Targets
Recptor

Other Targets
Research Area

Cancer
Indication

Breast Cancer

CAS Number

1256565-36-2
Formula Weight

467.346
Molecular Formula

C25H20Cl2N2O3
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 50 mg/mL (106.99 mM)
SMILES

COC1=CC=C(C=C1)C2C3=C(CCN2C(=O)OC4=CC=C(C=C4)Cl)C5=C(N3)C=CC(=C5)Cl
Chemical Name

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

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

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