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

Talotrexin  (Synonyms: PT523)

目录号: HY-10824 纯度: 99.27%
Data Sheet SDS COA 产品使用指南 技术支持

溶解度

动物溶解方案

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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1 mg ￥2200
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5 mg ￥5500
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Customer Review

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
NCT NumberSponsorConditionStart DatePhase
NCT00088023Spectrum Pharmaceuticals, Inc|National Cancer Institute (NCI)
Neoplasms
March 2004Phase 1
NCT00112060Spectrum Pharmaceuticals, Inc
Non-Small-Cell Lung Carcinoma
April 2008Phase 1|Phase 2
NCT00458744Children´s Oncology Group|National Cancer Institute (NCI)
Brain and Central Nervous System Tumors|Leukemia|Lymphoma|Unspecified Childhood Solid Tumor, Protocol Specific
February 2007Phase 1
分子量

573.56

Formula

C27H27N9O6
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (217.94 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7435 mL 8.7175 mL 17.4350 mL
5 mM 0.3487 mL 1.7435 mL 3.4870 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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动物溶解方案

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
纯度 & 产品资料
参考文献

Talotrexin 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7435 mL 8.7175 mL 17.4350 mL 43.5874 mL
5 mM 0.3487 mL 1.7435 mL 3.4870 mL 8.7175 mL
10 mM 0.1743 mL 0.8717 mL 1.7435 mL 4.3587 mL
15 mM 0.1162 mL 0.5812 mL 1.1623 mL 2.9058 mL
20 mM 0.0872 mL 0.4359 mL 0.8717 mL 2.1794 mL
25 mM 0.0697 mL 0.3487 mL 0.6974 mL 1.7435 mL
30 mM 0.0581 mL 0.2906 mL 0.5812 mL 1.4529 mL
40 mM 0.0436 mL 0.2179 mL 0.4359 mL 1.0897 mL
50 mM 0.0349 mL 0.1743 mL 0.3487 mL 0.8717 mL
60 mM 0.0291 mL 0.1453 mL 0.2906 mL 0.7265 mL
80 mM 0.0218 mL 0.1090 mL 0.2179 mL 0.5448 mL
100 mM 0.0174 mL 0.0872 mL 0.1743 mL 0.4359 mL

Keywords:

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

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目录号：
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