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Chemical Structure| 152946-68-4 Chemical Structure| 152946-68-4

Structure of Nolatrexed 2HCl
CAS No.: 152946-68-4

Chemical Structure| 152946-68-4

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Nolatrexed, also known as AG337, is a thymidylate synthase inhibitor with potential anticancer activity. A phase II study of nolatrexed in 2007 in advanced HCC patients demonstrated minimal activity and significant stomatitis. Hence, it does not warrant further study as a single agent for this disease.

Synonyms: AG 337; Thymitaq; Nolatrexed (hydrochloride)

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Product Details of Nolatrexed 2HCl

CAS No. :152946-68-4
Formula : C14H14Cl2N4OS
M.W : 357.26
SMILES Code : O=C1N=C(N)NC2=C1C(SC3=CC=NC=C3)=C(C)C=C2.[H]Cl.[H]Cl
Synonyms :
AG 337; Thymitaq; Nolatrexed (hydrochloride)
MDL No. :MFCD00917041

Safety of Nolatrexed 2HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H341-H361
Precautionary Statements:P201-P202-P280-P308+P313-P405-P501

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
L1210 cells 1 µM 16 hours Evaluate the potentiation of 5-FU cytotoxicity by NU3076 and dipyridamole. Results showed significant potentiation at high concentrations of 5-FU (30 µM and 100 µM). Br J Cancer. 1999 Aug;80(11):1738-46
L1210 cells 10 µM 16 hours Evaluate the potentiation of nolatrexed cytotoxicity by NU3076 and dipyridamole. Results showed that 1 µM NU3076 and 1 µM dipyridamole significantly reduced the LC90 by > threefold. Br J Cancer. 1999 Aug;80(11):1738-46
WiDr B 2.70 µM 72 hours To evaluate the anti-proliferative effects of Nolatrexed on WiDr B cells, IC50 value was 2.70 µM Br J Cancer. 2007 Mar 12;96(5):769-75
WiDr T 2.30 µM 72 hours To evaluate the anti-proliferative effects of Nolatrexed on WiDr T cells, IC50 value was 2.30 µM Br J Cancer. 2007 Mar 12;96(5):769-75
Lovo li 2.10 µM 72 hours To evaluate the anti-proliferative effects of Nolatrexed on Lovo li cells, IC50 value was 2.10 µM, showing higher sensitivity compared to Lovo 92 cells Br J Cancer. 2007 Mar 12;96(5):769-75
Lovo 175X2 19.00 µM 72 hours To evaluate the anti-proliferative effects of Nolatrexed on Lovo 175X2 cells, IC50 value was 19.00 µM, showing 3-fold resistance compared to Lovo 92 cells Br J Cancer. 2007 Mar 12;96(5):769-75
Lovo 92 5.15 µM 72 hours To evaluate the anti-proliferative effects of Nolatrexed on Lovo 92 cells, IC50 value was 5.15 µM Br J Cancer. 2007 Mar 12;96(5):769-75

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.80mL

0.56mL

0.28mL

14.00mL

2.80mL

1.40mL

27.99mL

5.60mL

2.80mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
 

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