2. Cell Cycle/DNA Damage Anti-infection Stem Cell/Wnt JAK/STAT Signaling
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  4. Cycloguanil hydrochloride

Cycloguanil (hydrochloride)  (Synonyms: シクログアニル塩酸塩; クロログアニドトリアジン塩酸塩)

製品番号: HY-12784A 純度: 99.93%
COA 取扱説明書 Technical Support

Cycloguanil (Chlorguanide triazine) hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.

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Cycloguanil hydrochloride

Cycloguanil (hydrochloride) 構造式

CAS 番号 : 152-53-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 44 在庫あり
Solution
10 mM * 1 mL in DMSO USD 44 在庫あり
Solid
5 mg $40 在庫あり
10 mg $57 在庫あり
25 mg $92 在庫あり
50 mg $130 在庫あり
100 mg $180 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

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Based on 3 publication(s) in Google Scholar

Other Forms of Cycloguanil hydrochloride:

Cycloguanil (hydrochloride) 関連抗体

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製品説明

Cycloguanil (Chlorguanide triazine) hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity[1][2].

IC50 & Target

Plasmodium

 

Cellular Effect
Cell Line Type Value Description References
Huh-7 CC50
27.36 3
Compound: GNF-Pf-2519
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
[PMID: 18579783]
Huh-7 CC50
27.36 3
Compound: GNF-Pf-2519
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
[PMID: 18579783]
体外実験

Cycloguanil hydrochloride exhibits anticancer activity against the NCI-60 panel of human tumor cell lines, and shows selective activity toward the MDA-MB-468 and MCF-7 breast cancer cell lines[2].
Cycloguanil (72 h) hydrochloride induces growth arrest in MDA-MB-468, MDA-MB-231 and MCF-7 breast cancer cells, with cell viability maintained at approximately 50% of that in the vehicle control group at high concentrations, and this effect cannot be reversed by folinic acid treatment[2].
Cycloguanil (0.001-10 μM; 24 h) hydrochloride binds to DHFR in intact MDA-MB-468 breast cancer cells, resulting in a dose-dependent accumulation of DHFR protein after 24 hours of treatment[2].
Cycloguanil (10 μM; 24 h) hydrochloride disrupts folate metabolism and nucleotide homeostasis in MDA-MB-231 breast cancer cells, and supplementation with Folinic acid (HY-17556) reverses the metabolite changes induced by it, a result consistent with DHFR inhibition[2].
Cycloguanil (0.02-20 μM; 6 h) hydrochloride potently inhibits the transcriptional activity of STAT3 in U3A fibrosarcoma cells at concentrations as low as 0.02 μM, which is consistent with the downstream effects of DHFR inhibition[2].

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

Cycloguanil (hydrochloride) 関連抗体

Western Blot Analysis[2]

Cell Line: MDA-MB-468 human breast cancer cells
Concentration: 0.001, 0.01, 0.1, 1 and 10 μM
Incubation Time: 24 h
Result: Induced a dose-dependent accumulation of DHFR protein, with increasing fold-change in DHFR levels observed across the tested concentration range.
分子量

288.18

分子式

C11H15Cl2N5
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC(N)=NC(C)(N1C2=CC=C(C=C2)Cl)C.[H]Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

DMSO : 62.5 mg/mL (216.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 25 mg/mL (86.75 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4701 mL 17.3503 mL 34.7005 mL
5 mM 0.6940 mL 3.4701 mL 6.9401 mL
10 mM 0.3470 mL 1.7350 mL 3.4701 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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 (7.22 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 (7.22 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.
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).
純度とドキュメンテーション

純度: 99.93%

COA (247 KB) HNMR (246 KB) LCMS (93 KB)

取扱説明書 (2659 KB)
参考文献

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
H2O / DMSO 1 mM 3.4701 mL 17.3503 mL 34.7005 mL 86.7513 mL
5 mM 0.6940 mL 3.4701 mL 6.9401 mL 17.3503 mL
10 mM 0.3470 mL 1.7350 mL 3.4701 mL 8.6751 mL
15 mM 0.2313 mL 1.1567 mL 2.3134 mL 5.7834 mL
20 mM 0.1735 mL 0.8675 mL 1.7350 mL 4.3376 mL
25 mM 0.1388 mL 0.6940 mL 1.3880 mL 3.4701 mL
30 mM 0.1157 mL 0.5783 mL 1.1567 mL 2.8917 mL
40 mM 0.0868 mL 0.4338 mL 0.8675 mL 2.1688 mL
50 mM 0.0694 mL 0.3470 mL 0.6940 mL 1.7350 mL
60 mM 0.0578 mL 0.2892 mL 0.5783 mL 1.4459 mL
80 mM 0.0434 mL 0.2169 mL 0.4338 mL 1.0844 mL
DMSO 100 mM 0.0347 mL 0.1735 mL 0.3470 mL 0.8675 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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Cycloguanil hydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

Cycloguanil152-53-4Chlorguanide triazineAntifolateParasiteDNA/RNA SynthesisSTATmalaria schizontserythrocyteshuman DHFRMDA-MB-468folate metabolismhepatocytesSTAT3primary human hepatocytesOCT1nucleotide metabolismInhibitorinhibitorinhibit

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