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Antifolate C2

Catalog No. T26636 CAS 1286279-90-0

Synonyms: AGF 154, AGF154, AGF-154

Antifolate C2 (AGF 154) has antitumor activity with an IC of 0.14 nM measured in a growth inhibition assay of human tumor cells.Antifolate C2 can be used for the study of cancer and autoimmune diseases.

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

Antifolate C2, CAS 1286279-90-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 350.00
5 mg	In stock	$ 828.00
10 mg	In stock	$ 1,130.00
25 mg	In stock	$ 1,590.00
50 mg	In stock	$ 1,980.00
100 mg	In stock	$ 2,500.00

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Purity: 98.63%

ee: 100%

Biological Description

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Description

In vivo

Antifolate C2 (AGF154) was synthesized as a potential antitumor agent. AGF154 inhibited the proliferation of Chinese hamster ovary (CHO) sublines expressing folate receptors (FRs) α or β (IC50s < 1 nM) or the proton-coupled folate transporter (PCFT) (IC50 < 7 nM). AGF154 inhibited KB, IGROV1, and SKOV3 human tumor cells at subnanomolar concentrations, reflecting both FRα and PCFT uptake. AGF154 inhibited glycinamide ribonucleotide formyltransferase (GARFTase). In severe combined immunodeficient mice bearing SKOV3 tumors, AGF154 was efficacious. The selectivity of AGF154 for PCFT and for FRα and β over the ubiquitously expressed reduced folate carrier is a paradigm for selective tumor targeting.[1]

Synonyms	AGF 154, AGF154, AGF-154
Molecular Weight	447.46
Formula	C19H21N5O6S
CAS No.	1286279-90-0

Storage

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

References and Literature

1. Wang L, et al. 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors. J Med Chem. 2015 Sep 10;58(17):6938-59. 2. Hou Z, et al. Dual Targeting of Epithelial Ovarian Cancer Via Folate Receptor α and the Proton-Coupled Folate Transporter with 6-Substituted Pyrrolo[2,3-d]pyrimidine Antifolates. Mol Cancer Ther. 2017 May;16(5):819-830. 3. Wilson M R, et al. Targeted therapy of non-small cell lung cancer (NSCLC) by novel 6-pyrrolo [2, 3-d] pyrimidine thienoyl antifolates with selective transport by the proton-coupled folate transporter (PCFT). Cancer Research.2015, 75(15_Supplement): 5403-5403. 4. Matherly LH, et al. Biology and therapeutic applications of the proton-coupled folate transporter. Expert Opin Drug Metab Toxicol. 2022 Oct;18(10):695-706.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library Anti-Cancer Compound Library Bioactive Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Antifolate C2 1286279-90-0 Others AGF 154 AGF154 AGF-154 Antifolate C-2 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.