Talotrexin
Based on 1 Customer Validation
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.
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- Purity : 99.27%
- CAS No.: 113857-87-7
- 화학식: C27H27N9O6
- 분자량:573.56
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
제품 설명
Cellular Effect
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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 |
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] |
| 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] |
| 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 |
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] |
| 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] |
| 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] |
| 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: 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: 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] |
In Vitro
Talotrexin shows no significant PCFT or FRα inhibitory activity[1].
Talotrexin (1-1000 nM) inhibits proliferation of R1-11/Tet-on-RFC HeLa cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSCLC xenografts in athymic female nude mice (6-8 weeks)[2]
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Dosage:15, 25, and 35 mg/kg, combined with Paclitaxel (HY-B0015, 7.5 mg/kg)
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Administration:IV injection, once weekly for 4 weeks
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Result:Inhibited A549 tumor growth.
Chemical Information
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CAS No. 113857-87-7
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Appearance Solid
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분자량 573.56
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화학식 C27H27N9O6
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Color Light yellow to yellow
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SMILES
NC1=NC(N)=NC2=C1N=C(CNC3=CC=C(C=C3)C(N[C@H](C(O)=O)CCCNC(C4=C(C=CC=C4)C(O)=O)=O)=O)C=N2
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Synonyms
PT523
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 125 mg/mL (217.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
순도&문서
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 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 |