Antifolate C2
Antifolate C2 is an anti-folate compound that has inhibitory effects on the proliferation of non-squamous non-small cell lung cancer (NS-NSCLC). Antifolate C2 achieves tumor selectivity by targeting proton-coupled folate transporter (PCFT), which is more selective to PCFT than the commonly used anti-folate drug Pemetrexed (HY-10820). Antifolate C2 blocks the biosynthesis of deoxypurine nucleotides by inhibiting glycinamide ribonucleotide formyltransferase (GARFTase), ultimately inhibiting the proliferation of tumor cells. Antifolate C2 can be used in studies of NS-NSCLC, especially in patients who do not respond well to Pemetrexed.
For research use only. We do not sell to patients.
- CAS No.: 1286279-90-0
- Formula: C19H21N5O6S
- Molecular Weight:447.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| IGROV-1 | IC50 |
0.77 nM
Compound: 7, AGF154
|
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 |
276 nM
Compound: 7, AGF154
|
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] |
| KB | IC50 |
0.09 nM
Compound: 7, AGF154
|
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 |
105 nM
Compound: 7, AGF154
|
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 |
2.6 nM
Compound: 7, AGF154
|
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] |
| R2 | IC50 |
290 nM
Compound: 7, AGF154
|
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 |
>1000 nM
Compound: 7, AGF154
|
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] |
| SK-OV-3 | IC50 |
15.5 nM
Compound: 7, AGF154
|
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 |
76 nM
Compound: 7, AGF154
|
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
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CAS No. 1286279-90-0
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Molecular Weight 447.46
-
Formula C19H21N5O6S
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SMILES
O=C1C2=C(NC(N)=N1)NC(CCCC3=CC(C(N[C@H](C(O)=O)CCC(O)=O)=O)=CS3)=C2
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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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)