2. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel Apoptosis
  3. Drug Metabolite P-glycoprotein Apoptosis
  4. N-Desmethyl imatinib

N-Desmethyl imatinib  (Synonyms: Norimatinib; Imatinib metabolite N-Desmethyl imatinib)

製品番号: HY-G0017 純度: 98.33%
COA 取扱説明書 Technical Support

N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia.

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N-Desmethyl imatinib

N-Desmethyl imatinib 構造式

CAS 番号 : 404844-02-6

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 232 在庫あり
Solution
10 mM * 1 mL in DMSO USD 232 在庫あり
Solid
1 mg $104 在庫あり
5 mg $220 在庫あり
10 mg $407 在庫あり
50 mg $1430 在庫あり
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Based on 1 publication(s) in Google Scholar

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N-Desmethyl imatinib 関連抗体

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製品説明

N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia[1][2][3].

体外実験

N-Desmethyl imatinib (CGP 74588) (0.3-30 μM) acts as a substrate for P-glycoprotein, stimulating ATPase activity in P-glycoprotein-expressing Sf9 cell membrane vesicles at concentrations ranging from 0.3 to 30 μM[3].
N-Desmethyl imatinib (48 h) inhibits K562 cell proliferation with an IC50 of 0.58 μM and shows no significant inhibition of K562/Dox cell proliferation (IC50 > 20 μM) after 48 h of treatment[3].
N-Desmethyl imatinib (1.6 μM, 20 μM; 48 h) induces apoptosis in K562 cells, but does not significantly induce apoptosis in K562/Dox cells[3].

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

N-Desmethyl imatinib 関連抗体

Cell Proliferation Assay[3]

Cell Line: human chronic myelogenous leukemia K562 cells, K562/Dox cells
Concentration: 0.1, 0.2, 0.4, 0.8, 1.6, 3.0 μM (K562 cells); 1, 2, 5, 10, 20 μM (K562/Dox cells)
Incubation Time: 48 h
Result: Inhibited K562 cell proliferation with an IC50 of 0.58 μM.
Showed no substantial proliferation inhibition in K562/Dox cells, with an IC50 greater than 20 μM.

Apoptosis Analysis[3]

Cell Line: human chronic myelogenous leukemia K562 cells, K562/Dox cells
Concentration: 1.6 μM (K562 cells); 20 μM (K562/Dox cells)
Incubation Time: 48 h
Result: Induced apoptosis in K562 cells, resulting in a hypoploid apoptotic population of 22.5%.
Did not induce a significant apoptotic response in K562/Dox cells, with a hypoploid population of 1.6% (similar to untreated control).
分子量

479.59

分子式

C28H29N7O
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC=C(C)C(NC2=NC(C3=CC=CN=C3)=CC=N2)=C1)C4=CC=C(CN5CCNCC5)C=C4
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (208.51 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 2.0851 mL 10.4256 mL 20.8511 mL
5 mM 0.4170 mL 2.0851 mL 4.1702 mL
10 mM 0.2085 mL 1.0426 mL 2.0851 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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  • Dilution Calculator

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

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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

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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: ≥ 2.5 mg/mL (5.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(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.
Please enter your animal formula composition:
%
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% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0851 mL 10.4256 mL 20.8511 mL 52.1279 mL
5 mM 0.4170 mL 2.0851 mL 4.1702 mL 10.4256 mL
10 mM 0.2085 mL 1.0426 mL 2.0851 mL 5.2128 mL
15 mM 0.1390 mL 0.6950 mL 1.3901 mL 3.4752 mL
20 mM 0.1043 mL 0.5213 mL 1.0426 mL 2.6064 mL
25 mM 0.0834 mL 0.4170 mL 0.8340 mL 2.0851 mL
30 mM 0.0695 mL 0.3475 mL 0.6950 mL 1.7376 mL
40 mM 0.0521 mL 0.2606 mL 0.5213 mL 1.3032 mL
50 mM 0.0417 mL 0.2085 mL 0.4170 mL 1.0426 mL
60 mM 0.0348 mL 0.1738 mL 0.3475 mL 0.8688 mL
80 mM 0.0261 mL 0.1303 mL 0.2606 mL 0.6516 mL
100 mM 0.0209 mL 0.1043 mL 0.2085 mL 0.5213 mL
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N-Desmethyl imatinib 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:

N-Desmethyl imatinib404844-02-6Norimatinib Imatinib metabolite N-Desmethyl imatinib CGP 74588CGP74588CGP 74588CGP-74588Drug MetaboliteP-glycoproteinApoptosisP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243gastrointestinal stromal tumorSARS-CoV-2CYP3A4K562/Dox cellschronic myeloid leukemiac-AblParkinson’s diseaseGIST patientsK562 cellsInhibitorinhibitorinhibit

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