2. Apoptosis
  3. Thymidylate Synthase
  4. Nolatrexed dihydrochloride

Nolatrexed dihydrochloride  (Synonyms: AG 337)

Cat. No.: HY-108474 Purity: 98.47%
COA
SDS
Handling Instructions Technical Support

Nolatrexed dihydrochloride (AG 337) is an orally active and non-competitive lipophilic inhibitor of thymidylate synthase with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride interacts at the folate cofactor binding site of the enzyme. Nolatrexed dihydrochloride increases sulfotransferases. Nolatrexed dihydrochloride induces cell cycle arrest in S phase of cancer cells. Nolatrexed dihydrochloride exhibits anticancer activity against cervical cancer.

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Nolatrexed dihydrochloride

Nolatrexed dihydrochloride 화학구조

CAS No. : 152946-68-4

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg   견적 받기  
200 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 2 publication(s) in Google Scholar

Other Forms of Nolatrexed dihydrochloride:

Nolatrexed dihydrochloride Related Antibodies

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Nolatrexed dihydrochloride

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Nolatrexed dihydrochloride (AG 337) is an orally active and non-competitive lipophilic inhibitor of thymidylate synthase with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride interacts at the folate cofactor binding site of the enzyme. Nolatrexed dihydrochloride increases sulfotransferases. Nolatrexed dihydrochloride induces cell cycle arrest in S phase of cancer cells. Nolatrexed dihydrochloride exhibits anticancer activity against cervical cancer.

IC50 & Target

Ki: 11 nM (Human Thymidylate Synthase)[1]
In Vitro

Nolatrexed (6-h exposure) dihydrochloride shows a certain inhibitory effect on CCRF-CEM cells in intermittent exposure[2].
Nolatrexed (1  nM-1.2  mM, 10 days) dihydrochloride significantly increases sulfotransferases expressions in HepG2 cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Nolatrexed dihydrochloride Related Antibodies
In Vivo

Nolatrexed (1-100 mg/kg, p.o., 2 weeks) dihydrochloride significantly increases sulfotransferases expressions in rat[3].
Nolatrexed dihydrochloride (50 mg/kg, i.v.) shows half-life, AUC, distribution factor and plasma clearance (CL) of 3.020 h, 89.972 mg/L/h, 0.831 L/kg, and 0.556 L/h/kg, respectively, in mice[4].
Nolatrexed dihydrochloride (200 mg/kg, p.o.) shows half-life, AUC, peak time (T(max)) and peak concentration (C(max)) for orally administered drug of 5.046 h, 84.893 mg/L/h, 1.000 h, and 18.0 mg/L, respectively, in mice[4].
Nolatrexed dihydrochloride (60 mg/m2; i.p.; every 4 h; 5 d) results in significant tumor growth retardation in nude mice bearing the HeLa Bu25TK- human cervical cell line[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
분자량

357.26

화학식

C14H14Cl2N4OS
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

[H]Cl.O=C1N=C(N)NC2=C1C(SC3=CC=NC=C3)=C(C)C=C2.[H]Cl
선적

Room temperature in continental US; may vary elsewhere.
보관

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

용액&용해도
In Vitro: 

DMSO : 50 mg/mL (139.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (139.95 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7991 mL 13.9954 mL 27.9908 mL
5 mM 0.5598 mL 2.7991 mL 5.5982 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 25 mg/mL (69.98 mM); Clear solution; Need ultrasonic and warming

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
순도&문서

Purity: 98.47%

SDS (419 KB)

COA (254 KB) HNMR (265 KB) LCMS (100 KB)

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 (sealed storage, away from moisture). 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 / H2O 1 mM 2.7991 mL 13.9954 mL 27.9908 mL 69.9770 mL
5 mM 0.5598 mL 2.7991 mL 5.5982 mL 13.9954 mL
10 mM 0.2799 mL 1.3995 mL 2.7991 mL 6.9977 mL
15 mM 0.1866 mL 0.9330 mL 1.8661 mL 4.6651 mL
20 mM 0.1400 mL 0.6998 mL 1.3995 mL 3.4989 mL
25 mM 0.1120 mL 0.5598 mL 1.1196 mL 2.7991 mL
30 mM 0.0933 mL 0.4665 mL 0.9330 mL 2.3326 mL
40 mM 0.0700 mL 0.3499 mL 0.6998 mL 1.7494 mL
50 mM 0.0560 mL 0.2799 mL 0.5598 mL 1.3995 mL
60 mM 0.0467 mL 0.2333 mL 0.4665 mL 1.1663 mL
80 mM 0.0350 mL 0.1749 mL 0.3499 mL 0.8747 mL
100 mM 0.0280 mL 0.1400 mL 0.2799 mL 0.6998 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Nolatrexed dihydrochloride 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:

Nolatrexed152946-68-4AG 337AG337AG-337Thymidylate SynthaseCCRF-CEMHepG2Inhibitorinhibitorinhibit

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상품명:
Nolatrexed dihydrochloride
Cat. No.:
HY-108474
수량:
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