Radiolabeled Antifolate Drug Acquisition

[3′, 5′, 7, 9-³H]Folic acid (25 Ci/mmol), [3′, 5′, 7-³H]MTX (20 Ci/mmol), and [¹⁴C(U)]-glycine (87mCi/mmol) were purchased from Moravek Biochemicals (Brea, CA). Unlabeled Folic acid was purchased from the Sigma-Aldrich (St. Louis, MO). LCV [(6R,S)5-formyl tetrahydrofolate] was provided by the Drug Development Branch, National Cancer Institute (Bethesda, MD). The sources of the classical antifolate drugs were as follows: MTX, Drug Development Branch, National Cancer Institute; LMTX (5,10-dideaza-5,6,7,8- tetrahydrofolate) and PMX [N-{4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5- yl)ethyl]benzoyl}-L-glutamic acid] (Alimta), Eli Lilly and Co. (Indianapolis, IN); RTX [N-(5-[N-(3,4- dihydro-2-methyl-4-oxyquinazolin-6-ylmethyl)-N-methyl-amino]-2-thienoyl)-L-glutamic acid], AstraZeneca Pharmaceuticals (Maccesfield, Cheshire, England); and PT523 [N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine],^{30 (link)} A. Rosowsky (Boston, MA). Other chemicals were obtained from commercial sources in the highest available purities.

Partial Protocol Preview
This section provides a glimpse into the protocol.
The remaining content is hidden due to licensing restrictions, but the full text is available at the following link: Access Free Full Text.

Golani L.K., Wallace-Povirk A., Deis S.M., Wong J.E., Ke J., Gu X., Raghavan S., Wilson M.R., Li X., Polin L., de Waal P.W., White K., Kushner J., O’Connor C., Hou Z., Xu H.E., Melcher K., Dann CE I.I.I., Matherly L.H, & Gangjee A. (2016). Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions Via Cellular Uptake by Folate Receptor α and the Proton-coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis. Journal of medicinal chemistry, 59(17), 7856-7876.

Publication 2016

Folic acid [14C(U)]-glycine Unlabeled folic acid

5 formyl tetrahydrofolate Alimta Antifolate Folic acid Glycine L glutamic acid Lmtx Ornithine Pharmaceuticals Pt523 Tetrahydrofolate

Corresponding Organization :

Other organizations : Duquesne University, The Barbara Ann Karmanos Cancer Institute, Indiana University Bloomington, Van Andel Institute, Wayne State University, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Institutes for Biological Sciences

Top 5 similar protocols

Variable analysis

independent variables

[3′, 5′, 7, 9-^3H]Folic acid (25 Ci/mmol)
[3′, 5′, 7-^3H]MTX (20 Ci/mmol)
[^14C(U)]-glycine (87mCi/mmol)
Unlabeled folic acid

dependent variables

Not explicitly mentioned

control variables

LCV [(6R,S)5-formyl tetrahydrofolate]
MTX (provided by the Drug Development Branch, National Cancer Institute)
LMTX (5,10-dideaza-5,6,7,8- tetrahydrofolate) (provided by Eli Lilly and Co.)
PMX [N-{4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5- yl)ethyl]benzoyl}-L-glutamic acid] (Alimta) (provided by Eli Lilly and Co.)
RTX [N-(5-[N-(3,4- dihydro-2-methyl-4-oxyquinazolin-6-ylmethyl)-N-methyl-amino]-2-thienoyl)-L-glutamic acid] (provided by AstraZeneca Pharmaceuticals)
PT523 [N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine] (provided by A. Rosowsky)

positive controls

LCV [(6R,S)5-formyl tetrahydrofolate]

negative controls

Not explicitly mentioned

Annotations

Based on most similar protocols

Etiam vel ipsum. Morbi facilisis vestibulum nisl. Praesent cursus laoreet felis. Integer adipiscing pretium orci. Nulla facilisi. Quisque posuere bibendum purus. Nulla quam mauris, cursus eget, convallis ac, molestie non, enim. Aliquam congue. Quisque sagittis nonummy sapien. Proin molestie sem vitae urna. Maecenas lorem.

As authors may omit details in methods from publication, our AI will look for missing critical information across the 5 most similar protocols.

About PubCompare

Our mission is to provide scientists with the largest repository of trustworthy protocols and intelligent analytical tools, thereby offering them extensive information to design robust protocols aimed at minimizing the risk of failures.

We believe that the most crucial aspect is to grant scientists access to a wide range of reliable sources and new useful tools that surpass human capabilities.

However, we trust in allowing scientists to determine how to construct their own protocols based on this information, as they are the experts in their field.

Ready to get started?

Revolutionizing how scientists
search and build protocols!