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Cat. No.: HY-175428

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Antifolate agent 1

Antifolate agent 1 is a 6-substituted pyrrolopyrimidine antifolate with a 1-carbon bridge. Antifolate agent 1 shows no activity against cells expressing FRα and FRβ, and has no GARFTase inhibitory activity. Antifolate agent 1 can be used as a negative control in the development of folate receptor-targeted antifolates.

For research use only. We do not sell to patients.

CAS No.: 518063-75-7
Formula: C₁₉H₁₉N₅O₆
Molecular Weight:413.38

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

Antifolate agent 1 Chemical Structure

CAS No.: 518063-75-7

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
IGROV-1	IC₅₀	>1000 nM Compound: 1	Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells	[PMID: 18680275]
IGROV-1	IC₅₀	>1000 nM Compound: 1	Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells in presence of folic acid Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells in presence of folic acid	[PMID: 18680275]
KB	IC₅₀	>1000 nM Compound: 1	Antiproliferative activity against human RFC and FRalpha expressing human KB cells Antiproliferative activity against human RFC and FRalpha expressing human KB cells	[PMID: 18680275]
KB	IC₅₀	>1000 nM Compound: 1	Antiproliferative activity against human RFC and FRalpha expressing human KB cells in presence of folic acid Antiproliferative activity against human RFC and FRalpha expressing human KB cells in presence of folic acid	[PMID: 18680275]
KB	IC₅₀	>1000 nM Compound: 1	Inhibition of GARFTase in human KB cells assessed as inhibition of [14C]glycine incorporation into [14C]formylGAR in presence of azaserine Inhibition of GARFTase in human KB cells assessed as inhibition of [14C]glycine incorporation into [14C]formylGAR in presence of azaserine	[PMID: 18680275]
R2	IC₅₀	>1000 nM Compound: 1	Antiproliferative activity against human RFC expressing Chinese hamster R2 cells Antiproliferative activity against human RFC expressing Chinese hamster R2 cells	[PMID: 18680275]

In Vitro

Antifolate agent 1 (Compound 1) (0-1000 nM; 0-96 h) does not inhibit the proliferation of RFC-expressing PC43-10 CHO cells, RFC- and FR-deficient R2 CHO cells, FRα-expressing RT16 CHO cells, FRβ-expressing D4 CHO cells, FRα-expressing KB human cervical cancer cells, or FRα-expressing IGROV1 human ovarian cancer cells^[1].
Antifolate agent 1 (10 μM; 2 min) acts as a weak inhibitor of RFC-mediated [³H]MTX uptake in PC43-10 CHO cells, reducing the uptake by less than 20%^[1].
Antifolate agent 1 (0-000 nM; 15.5 h) does not inhibit in situ GARFTase activity in KB human cervical cancer cells, with an IC₅₀ greater than 1000 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

RFC-expressing PC43-10 CHO cells, RFC- and FR-null R2 CHO cells, FRα-expressing RT16 CHO cells, FRβ-expressing D4 CHO cells, FRα-expressing KB human cervical cancer cells, FRα-expressing IGROV1 human ovarian cancer cells
Concentration:

0-1000 nM
Incubation Time:

up to 96 h
Result:

Exhibited an IC₅₀ > 1000 nM in PC43-10 cells, R2 cells, RT16 cells, D4 cells, KB cells and IGROV1 cells, with IC₅₀ remaining > 1000 nM in the presence of 200 nM folic acid.

Chemical Information

CAS No. 518063-75-7
Molecular Weight 413.38
Formula C₁₉H₁₉N₅O₆
SMILES

O=C1C2=C(NC(N)=N1)NC(CC3=CC=C(C=C3)C(N[C@H](C(O)=O)CCC(O)=O)=O)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Deng Y, et al. Synthesis and discovery of high affinity folate receptor-specific glycinamide ribonucleotide formyltransferase inhibitors with antitumor activity. J Med Chem. 2008;51(16):5052-5063. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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