2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. Antifolate Dihydrofolate reductase (DHFR)
  4. Talotrexin

Talotrexin (PT523) 是一种 Aminopterin (HY-14518) 的类似物，是一种非聚谷氨酸化的经典抗叶酸剂 (antifolate)。 Talotrexin 是一种 RFC (还原型叶酸载体)的特异性抑制剂，可选择性地抑制 RFC 转运。Talotrexin 通过靶向 DHFR 抑制肿瘤生长显示出抗肿瘤活性。

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Talotrexin Chemical Structure

Talotrexin Chemical Structure

CAS No. : 113857-87-7

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Other Forms of Talotrexin:

Talotrexin 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

Talotrexin (PT523), an analog of Aminopterin (HY-14518), is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
IGROV-1 IC50
2.47 nM
Compound: 8, PT523
Growth inhibition of human IGROV1 cells expressing RFC, FRalpha and PCFT in presence of 200 nM folic acid after 96 hrs
Growth inhibition of human IGROV1 cells expressing RFC, FRalpha and PCFT in presence of 200 nM folic acid after 96 hrs
[PMID: 20085328]
IGROV-1 IC50
2.47 nM
Compound: 9, PT523
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
3.47 nM
Compound: 9, PT523
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
3.47 nM
Compound: 8, PT523
Growth inhibition of human IGROV1 cells expressing RFC, FRalpha and PCFT after 96 hrs
Growth inhibition of human IGROV1 cells expressing RFC, FRalpha and PCFT after 96 hrs
[PMID: 20085328]
KB IC50
2.9 nM
Compound: 8, PT523
Growth inhibition of human KB cells expressing RFC, FRalpha and PCFT in presence of 200 nM folic acid after 96 hrs
Growth inhibition of human KB cells expressing RFC, FRalpha and PCFT in presence of 200 nM folic acid after 96 hrs
[PMID: 20085328]
KB IC50
2.9 nM
Compound: 9, PT523
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
5.26 nM
Compound: 9, PT523
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
5.26 nM
Compound: 8, PT523
Growth inhibition of human KB cells expressing RFC, FRalpha and PCFT after 96 hrs
Growth inhibition of human KB cells expressing RFC, FRalpha and PCFT after 96 hrs
[PMID: 20085328]
R2 IC50
> 1000 nM
Compound: 9, PT523
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
> 1000 nM
Compound: 9, PT523
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
> 1000 nM
Compound: 8, PT523
Growth inhibition of Chinese hamster R2 cells expressing human RFC after 96 hrs
Growth inhibition of Chinese hamster R2 cells expressing human RFC after 96 hrs
[PMID: 20085328]
R2 IC50
> 1000 nM
Compound: 8, PT523
Growth inhibition of Chinese hamster R2 cells expressing human RFC and human PCFT4 after 96 hrs
Growth inhibition of Chinese hamster R2 cells expressing human RFC and human PCFT4 after 96 hrs
[PMID: 20085328]
体外研究
(In Vitro)

Talotrexin 未显示出显著的 PCFT 或 FRα 抑制活性[1]。
Talotrexin (1-1000 nM) 可抑制 R1-11/Tet-on-RFC HeLa 细胞的增殖[2]。

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

Talotrexin 相关抗体:
体内研究
(In Vivo)

Talotrexin (0-35 mg/kg，静脉注射，每周一次，持续 4 周) 单独或与Paclitaxel (HY-B0015, 7.5 mg/kg) 联合使用可抑制小鼠 A549 肿瘤的生长[2]。

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

Animal Model: NSCLC xenografts in athymic female nude mice (6-8 weeks)[2]
Dosage: 15, 25, and 35 mg/kg, combined with Paclitaxel (HY-B0015, 7.5 mg/kg)
Administration: IV injection, once weekly for 4 weeks
Result: Inhibited A549 tumor growth.
Clinical Trial
分子量

573.56

Formula

C27H27N9O6
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

Talotrexin 相关分类

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  • 稀释计算器

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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:

Talotrexin113857-87-7PT523PT 523PT-523AntifolateDihydrofolate reductase (DHFR)R1-11Tet-on-RFCHeLa cellsDHFRreduced folate carrierantifolateNSCLCA549 tumorInhibitorinhibitorinhibit

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