Antifolate C2

Cat. No.: HY-126830: FAQs
Data Sheet Handling Instructions

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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.

Antifolate C2 Chemical Structure

CAS No. : 1286279-90-0

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Description

Cellular Effect

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	> 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]
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]
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]

Molecular Weight

447.46

Formula

C₁₉H₂₁N₅O₆S

CAS No.

1286279-90-0

SMILES

O=C1C2=C(NC(N)=N1)NC(CCCC3=CC(C(N[C@H](C(O)=O)CCC(O)=O)=O)=CS3)=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

Handling Instructions (2659 KB)

References

[1]. Wilson M R, et al. Targeting nonsquamous nonsmall cell lung cancer via the proton-coupled folate transporter with 6-substituted pyrrolo [2, 3-d] pyrimidine thienoyl antifolates[J]. Molecular pharmacology, 2016, 89(4): 425-434. [Content Brief]

Antifolate C2 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Antifolate C21286279-90-0Antifolate C 2Antifolate C-2AntifolateApoptosisantifolicsNS-NSCLCGARFTPCFTtumor cell proliferationInhibitorinhibitorinhibit

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