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PTC299

Catalog No. T12574 CAS 1256565-36-2

Synonyms: Emvododstat, (4-chlorophenyl) (1S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxylate

PTC299 ((4-chlorophenyl) (1S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxylate) is an orally active inhibitor of VEGFA mRNA translation and selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydrolactate dehydrogenase (DHODH).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PTC299, CAS 1256565-36-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 119.00
5 mg	In stock	$ 255.00
10 mg	In stock	$ 389.00
25 mg	In stock	$ 655.00
50 mg	In stock	$ 932.00
100 mg	In stock	$ 1,270.00
1 mL * 10 mM (in DMSO)	In stock	$ 263.00

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Purity: 99.19%

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Description

In vitro

PTC299 as an inhibitor of VEGFA mRNA translation in a phenotypic screen and evaluated in the clinic for treatment of solid tumors. To guide precision cancer treatment, we performed extensive biological characterization of the activity of PTC299 and demonstrated that inhibition of VEGF production and cell proliferation by PTC299 is linked to a decrease in uridine nucleotides by targeting dihydroorotate dehydrogenase (DHODH), a rate-limiting enzyme for de novo pyrimidine nucleotide synthesis.

Synonyms	Emvododstat, (4-chlorophenyl) (1S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxylate
Molecular Weight	467.34
Formula	C25H20Cl2N2O3
CAS No.	1256565-36-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (106.99 mM), Sonication is recommended.

References and Literature

1. Cao L, et al. Targeting of Hematologic Malignancies with PTC299, A Novel Potent Inhibitor of DihydroorotateDehydrogenase with Favorable Pharmaceutical Properties. Mol Cancer Ther. 2019 Jan;18(1):3-16. 2. Bender Ignacio RA, et al. Brief Report: A Phase 1b/Pharmacokinetic Trial of PTC299, a Novel PostTranscriptional VEGF Inhibitor, for AIDS-Related Kaposi's Sarcoma: AIDS Malignancy Consortium Trial 059. J Acquir Immune Defic Syndr. 2016 May 1;72(1):52-7. 3. Zeng Z, et al, Targeting dihydroorotate dehydrogenase in acute myeloid leukemia. Haematologica. 2018 Sep;103(9):1415-1417.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Inhibitor Library Drug Repurposing Compound Library Orally Active Compound Library Clinical Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

PTC299 1256565-36-2 Angiogenesis Metabolism Tyrosine Kinase/Adaptors Dehydrogenase VEGFR hematologic Vascular endothelial growth factor receptor cancer Inhibitor myelosuppression Emvododstat off-target DHODH DNA/RNA Synthesis Dihydroorotate Dehydrogenase PTC 299 kinase (4-chlorophenyl) (1S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxylate oral inhibit malignancies PTC-299 inhibitor

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