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Art. -Nr.: HY-10824

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Talotrexin

(Synonyms: PT523)

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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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Reinheit: 99.27%
CAS. Nr.: 113857-87-7
Formel: C₂₇H₂₇N₉O₆
Molecular Weight:573.56

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Talotrexin Chemical Structure

CAS. Nr.: 113857-87-7

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Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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	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.

In Vivo

Talotrexin (0-35 mg/kg, IV injection, once weekly for 4 weeks) alone or combined with Paclitaxel (HY-B0015, 7.5 mg/kg) inhibits A549 tumor growth in mice^[2].

MedChemExpress (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.

Chemical Information

CAS. Nr. 113857-87-7
Appearance Solid
Molecular Weight 573.56
Formel C₂₇H₂₇N₉O₆
Color Light yellow to yellow
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
Synonyms

PT523
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7435 mL

8.7175 mL

17.4350 mL

5 mM

0.3487 mL

1.7435 mL

3.4870 mL

10 mM

0.1743 mL

0.8717 mL

1.7435 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. O'Connor C, et al. Folate transporter dynamics and therapy with classic and tumor-targeted antifolates. Sci Rep. 2021 Mar 18;11(1):6389. [Content Brief]

[2]. Choy G S, et al. Combination talotrexin (PT-523) with paclitaxel in A549 non-small cell lung cancer (NSCLC) athymic nude mice xenografts[J]. Cancer Research, 2007, 67(1_Annual_Meeting).

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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Talotrexin

MCE Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Talotrexin Related Classifications

HY-10824 Related Classifications