Antifolates are compounds that antagonise the actions of folic acid (vitamin B9). Folic acid's primary function in the body is as a cofactor to various methyltransferases involved in serine, methionine, thymidine and purine biosynthesis. Consequently antifolates inhibit cell division, DNA/RNA synthesis and repair and protein synthesis. Some such as Proguanil, Pyrimethamine and Trimethoprim selectively inhibit folate's actions in microbial organisms such as bacteria, protozoa and fungi. The majority of antifolates work by inhibiting dihydrofolate reductase (DHFR). Many are primarily DHFR inhibitors, but Raltitrexed is an inhibitor of thymidylate synthase, and Pemetrexed inhibits both and a third enzyme. Antifolates act specifically during DNA and RNA synthesis, and thus are cytotoxic during the S-phase of the cell cycle. Thus, they have a greater toxic effect on rapidly dividing cells.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H8842 |
Fanotaprim |
2120282-75-7 | Fanotaprim is a a selective and potent TgDHFR inhibitor,has a TgDHFR IC50 of 1.57 ± 0.11 nM and a hDHFR to TgDHFR selectivity ratio of 196. |
H1834 |
Trimetrexate |
52128-35-5 | A quinazoline derivative and antifolate agent that fuctions as a dihydrofolate reductase (DHFR) inhibitor; shows activity against transport-deficient MTX-resistant tumor cells that overcome the acquired and natural resistance to methotrexate. |
H1833 |
TNP-351 |
125991-51-7 | TNP-351 is an antifolate compound that functions as a DHFR inhibitor, strongly inhibits the growth of Meth A cells. |
H1832 |
Pralatrexate |
146464-95-1 | An antifolate that fuctions as a dihydrofolate reductase inhibitor for treatment of several malignancies. |
H1831 |
Pemetrexed disodium |
150399-23-8 | A classical multitargeted antifolate that inhibits multiple folate-requiring enzymes TS/DHFR/GARFT with Ki of 1.3/7.2/65 nM respectively; increases the cytotoxicity and antitumor activity of gemcitabine in HT29 colon carcinoma. |
H1830 |
Pemetrexed |
137281-23-3 | A classical multitargeted antifolate that inhibits multiple folate-requiring enzymes TS/DHFR/GARFT with Ki of 1.3/7.2/65 nM respectively; increases the cytotoxicity and antitumor activity of gemcitabine in HT29 colon carcinoma. |
H1829 |
LSN 3213128 |
1941211-99-9 | LSN 3213128 is a novel potent, selective and orally-bioavailable antifolate with potent and specific inhibitory activity for AICARFT; results in dramatic elevation of 5-aminoimidazole 4-carboxamide ribonucleotide (ZMP) and growth inhibition in NCI-H460 and MDA-MB-231met2 cancer cell lines; demonstrates tumor growth inhibition in a murine based xenograft model of triple negative breast cancer (TNBC); Aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT) is an enzyme in the purine biosynthetic pathway. |
H1828 |
Levomefolate calcium |
151533-22-1 | A calcium salt of levomefolic acid. |
H1827 |
Calcium N5-methyltetrahydrofolate |
26560-38-3 | The calcium salt of levomefolic acid that has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers. |
H1826 |
Arfolitixorin |
31690-11-6 | Arfolitixorin is a novel antifolate modulator compound. |
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