2. Cell Cycle/DNA Damage Apoptosis
  3. Antifolate Apoptosis
  4. Antifolate C2

Antifolate C2 是一种抗叶酸化合物，对非鳞状非小细胞肺癌 (NS-NSCLC) 的增殖有抑制效果。Antifolate C2 通过靶向质子偶联叶酸转运蛋白 (PCFT) 实现对肿瘤的选择性作用，与常用的抗叶酸药物 Pemetrexed (HY-10820) 相比，Antifolate C2 对 PCFT 具有更高的选择性。Antifolate C2 通过抑制甘氨酰胺核糖核苷酸甲酰转移酶 (GARFTase) 来阻断脱氧嘌呤核苷酸的生物合成，最终抑制肿瘤细胞的增殖。Antifolate C2 可以用于 NS-NSCLC 的研究，尤其是对于那些对 Pemetrexed 反应不佳的患者。

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Antifolate C2 Chemical Structure

Antifolate C2 Chemical Structure

CAS No. : 1286279-90-0

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Antifolate C2 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

细胞效力
(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]
分子量

447.46

Formula

C19H21N5O6S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Antifolate C2 相关分类

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  • 稀释计算器

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (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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