Talotrexin (Synonyms: PT523)

Name: Talotrexin
Brand: MedChemExpress
SKU: HY-10824
Rating: 4.5 (1 reviews)

Cat. No.: HY-10824 Purity: 99.27%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

Talotrexin Chemical Structure

CAS No. : 113857-87-7

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Talotrexin:

Talotrexin monoammonium Get quote
Talotrexin ammonium Get quote

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Biological Activity
Purity & Documentation
References
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Description

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]

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.

Clinical Trial

Molecular Weight

573.56

Formula

C₂₇H₂₇N₉O₆

CAS No.

113857-87-7

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.1743 mL	0.8717 mL	1.7435 mL

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.27%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (248 KB) HNMR (458 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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).

Complete Stock Solution Preparation Table

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

Talotrexin Related Classifications

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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Talotrexin (Synonyms: PT523)

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Complete Stock Solution Preparation Table

Talotrexin Related Classifications

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