Cat. No.: HY-123751

Antifolate C1

(Synonyms: AGF 94)

Antifolate C1 (AGF 94) is a GARFTase inhibitor. Antifolate C1 inhibits de novo purine biosynthesis. Antifolate C1 inhibits cell proliferation.

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CAS No.: 136784-51-5
Formula: C₁₉H₂₁N₅O₆S
Molecular Weight:447.46

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

Data Sheet (265 KB)

Antifolate C1 Chemical Structure

CAS No.: 136784-51-5

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Biological Activity
- Description
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
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Biological Activity

Description

Antifolate C1 (AGF 94) is a GARFTase inhibitor. Antifolate C1 inhibits de novo purine biosynthesis. Antifolate C1 inhibits cell proliferation^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	27.4 nM Compound: 1	Antiproliferative activity against human A2780 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against human A2780 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	0.55 nM Compound: 3	Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
IGROV-1	IC₅₀	>1000 nM Compound: 3	Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid	[PMID: 21879757]
IGROV-1	IC₅₀	0.55 nM Compound: 3a	Growth inhibition of human IGROV1 cells endogenously expressing RFC/FRalpha/PCFT incubated for 96 hrs by CellTiter-blue cell viability assay Growth inhibition of human IGROV1 cells endogenously expressing RFC/FRalpha/PCFT incubated for 96 hrs by CellTiter-blue cell viability assay	[PMID: 22243528]
IGROV-1	IC₅₀	>1000 nM Compound: 3a	Growth inhibition of human IGROV1 cells endogenously expressing RFC/FRalpha/PCFT in presence of folic acid incubated for 96 hrs by CellTiter-blue cell viability assay Growth inhibition of human IGROV1 cells endogenously expressing RFC/FRalpha/PCFT in presence of folic acid incubated for 96 hrs by CellTiter-blue cell viability assay	[PMID: 22243528]
IGROV-1	IC₅₀	0.73 nM Compound: 4, AGF94	Antiproliferative activity against human IGROV1 cells after 96 hrs by CellTiter-Blue assay Antiproliferative activity against human IGROV1 cells after 96 hrs by CellTiter-Blue assay	[PMID: 26317331]
IGROV-1	IC₅₀	126 nM Compound: 4, AGF94	Antiproliferative activity against human IGROV1 cells after 96 hrs by CellTiter-Blue assay in presence of 200 nM folic acid Antiproliferative activity against human IGROV1 cells after 96 hrs by CellTiter-Blue assay in presence of 200 nM folic acid	[PMID: 26317331]
IGROV-1	IC₅₀	0.95 nM Compound: 3	Antiproliferative activity against human IGROV1 cells expressing human FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue fluorescence analysis Antiproliferative activity against human IGROV1 cells expressing human FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue fluorescence analysis	[PMID: 27458733]
IGROV-1	IC₅₀	213 nM Compound: 3	Antiproliferative activity against human IGROV1 cells expressing human FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue fluorescence analysis Antiproliferative activity against human IGROV1 cells expressing human FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue fluorescence analysis	[PMID: 27458733]
IGROV-1	IC₅₀	0.27 μM Compound: 1	Anticlonogenic activity against human IGROV1 cells incubated for 24 hrs followed by compound wash out and measured after 10 days by methylene blue staining-based assay Anticlonogenic activity against human IGROV1 cells incubated for 24 hrs followed by compound wash out and measured after 10 days by methylene blue staining-based assay	[PMID: 29701475]
IGROV-1	IC₅₀	10.1 nM Compound: 1	Antiproliferative activity against human IGROV1 cells harboring non targeted control shRNA sequence after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against human IGROV1 cells harboring non targeted control shRNA sequence after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	16.7 nM Compound: 1	Antiproliferative activity against wild type human IGROV1 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against wild type human IGROV1 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	190 nM Compound: 1	Antiproliferative activity against FRalpha knockout human IGROV1 KD4 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against FRalpha knockout human IGROV1 KD4 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	74.6 nM Compound: 1	Antiproliferative activity against FRalpha knockout human IGROV1 KD10 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against FRalpha knockout human IGROV1 KD10 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
KB	IC₅₀	0.26 nM Compound: 3	Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
KB	IC₅₀	>1000 nM Compound: 3	Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid	[PMID: 21879757]
KB	IC₅₀	0.26 nM Compound: 3a	Growth inhibition of human KB cells endogenously expressing RFC/FRalpha/PCFT incubated for 96 hrs by CellTiter-blue cell viability assay Growth inhibition of human KB cells endogenously expressing RFC/FRalpha/PCFT incubated for 96 hrs by CellTiter-blue cell viability assay	[PMID: 22243528]
KB	IC₅₀	>1000 nM Compound: 3a	Growth inhibition of human KB cells endogenously expressing RFC/FRalpha/PCFT in presence of folic acid incubated for 96 hrs by CellTiter-blue cell viability assay Growth inhibition of human KB cells endogenously expressing RFC/FRalpha/PCFT in presence of folic acid incubated for 96 hrs by CellTiter-blue cell viability assay	[PMID: 22243528]
KB	IC₅₀	0.26 nM Compound: 7	Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
KB	IC₅₀	2 nM Compound: 7	Inhibition of GARFTase in human KB cells assessed as reduction in [14C]glycine incorporation into [14C]formyl GAR incubated for 15 hrs by ion-exchange chromatography Inhibition of GARFTase in human KB cells assessed as reduction in [14C]glycine incorporation into [14C]formyl GAR incubated for 15 hrs by ion-exchange chromatography	[PMID: 25234128]
KB	IC₅₀	>1000 nM Compound: 7	Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs in presence of 200 nM folic acid by Celltiter-blue cell viability assay Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs in presence of 200 nM folic acid by Celltiter-blue cell viability assay	[PMID: 25234128]
KB	IC₅₀	0.26 nM Compound: 4, AGF94	Antiproliferative activity against human KB cells expressing FRalpha/PCFT/RFC assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assay Antiproliferative activity against human KB cells expressing FRalpha/PCFT/RFC assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assay	[PMID: 26317331]
KB	IC₅₀	101 nM Compound: 4, AGF94	Antiproliferative activity against human KB cells expressing FRalpha/PCFT/RFC assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assay in presence of 200 nM folic acid Antiproliferative activity against human KB cells expressing FRalpha/PCFT/RFC assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assay in presence of 200 nM folic acid	[PMID: 26317331]
KB	IC₅₀	3.5 nM Compound: 4, AGF94	Inhibition of GARFTase in human KB cells expressing FRalpha/PCFT/RFC assessed as incorporation of [14C(U)]-glycine into [14C]-formyl GAR preincubated for 1 hr followed by azaserine, L-glutamine, 14C(U)]-glycine addition measured after 16 hrs Inhibition of GARFTase in human KB cells expressing FRalpha/PCFT/RFC assessed as incorporation of [14C(U)]-glycine into [14C]-formyl GAR preincubated for 1 hr followed by azaserine, L-glutamine, 14C(U)]-glycine addition measured after 16 hrs	[PMID: 26317331]
KB	IC₅₀	101 nM Compound: 3	Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue fluorescence analysis Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue fluorescence analysis	[PMID: 27458733]
R2	IC₅₀	0.69 nM Compound: 3	Inhibition of GARFTase in chinese hamster R2 cells expressing human PCFT assessed as incorporation of [14C]glycine into [14C]formyl GAR in the presence of 4 uM azaserine Inhibition of GARFTase in chinese hamster R2 cells expressing human PCFT assessed as incorporation of [14C]glycine into [14C]formyl GAR in the presence of 4 uM azaserine	[PMID: 21879757]
R2	IC₅₀	1.4 nM Compound: 3	Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as inhibition of colony formation after 10 to 14 days Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as inhibition of colony formation after 10 to 14 days	[PMID: 21879757]
R2	IC₅₀	273.5 nM Compound: 3	Antiproliferative activity against chinese hamster R2 cells assessed as reduction of viable cells after 96 hrs Antiproliferative activity against chinese hamster R2 cells assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
R2	IC₅₀	3.34 nM Compound: 3	Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
R2	IC₅₀	273.5 nM Compound: 3a	Growth inhibition of Chinese hamster R2 cells deficient in reduced folate carrier and human folate receptor alpha incubated for 96 hrs by CellTiter-blue cell viability assay Growth inhibition of Chinese hamster R2 cells deficient in reduced folate carrier and human folate receptor alpha incubated for 96 hrs by CellTiter-blue cell viability assay	[PMID: 22243528]
R2	IC₅₀	288 nM Compound: 3a	Growth inhibition of Chinese hamster R2 cells expressing empty vector control incubated for 96 hrs by CellTiter-blue cell viability assay Growth inhibition of Chinese hamster R2 cells expressing empty vector control incubated for 96 hrs by CellTiter-blue cell viability assay	[PMID: 22243528]
R2	IC₅₀	3.34 nM Compound: 3a	Growth inhibition of Chinese hamster R2 cells expressing human PCFT incubated for 96 hrs by CellTiter-blue cell viability assay Growth inhibition of Chinese hamster R2 cells expressing human PCFT incubated for 96 hrs by CellTiter-blue cell viability assay	[PMID: 22243528]
R2	IC₅₀	273.5 nM Compound: 7	Cytotoxicity against Chinese hamster R2 cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against Chinese hamster R2 cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
R2	IC₅₀	288 nM Compound: 7	Cytotoxicity against Chinese hamster R2 cells expressing empty vector assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against Chinese hamster R2 cells expressing empty vector assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
R2	IC₅₀	273.5 nM Compound: 4, AGF94	Cytotoxicity against PCFT-null Chinese hamster R2 cells assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assay Cytotoxicity against PCFT-null Chinese hamster R2 cells assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assay	[PMID: 26317331]
R2	IC₅₀	288 nM Compound: 4, AGF94	Cytotoxicity against Chinese hamster R2 cells transfected with empty PCDNA3 assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assay Cytotoxicity against Chinese hamster R2 cells transfected with empty PCDNA3 assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assay	[PMID: 26317331]
R2	IC₅₀	249 nM Compound: 1	Antiproliferative activity in Chinese hamster R2 cells deficient in RFC, PCFT, and FRalpha assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Antiproliferative activity in Chinese hamster R2 cells deficient in RFC, PCFT, and FRalpha assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
SK-OV-3	IC₅₀	2.2 nM Compound: 4, AGF94	Antiproliferative activity against human SKOV3 cells after 96 hrs by CellTiter-Blue assay Antiproliferative activity against human SKOV3 cells after 96 hrs by CellTiter-Blue assay	[PMID: 26317331]
SK-OV-3	IC₅₀	47 nM Compound: 4, AGF94	Antiproliferative activity against human SKOV3 cells after 96 hrs by CellTiter-Blue assay in presence of 200 nM folic acid Antiproliferative activity against human SKOV3 cells after 96 hrs by CellTiter-Blue assay in presence of 200 nM folic acid	[PMID: 26317331]

Chemical Information

CAS No. 136784-51-5
Molecular Weight 447.46
Formula C₁₉H₂₁N₅O₆S
SMILES

O=C1C2=C(NC(N)=N1)NC(CCCC3=CC=C(C(N[C@H](C(O)=O)CCC(O)=O)=O)S3)=C2
Synonyms

AGF 94
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 (265 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]. O'Connor C, et al. Folate transporter dynamics and therapy with classic and tumor-targeted antifolates. Sci Rep. 2021 Mar 18;11(1):6389. [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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