1. PI3K/Akt/mTOR
  2. PI3K Akt
  3. Zandelisib

Zandelisib  (Synonyms: ME-401; PWT-143)

製品番号: HY-109198 純度: 99.67%
COA 取扱説明書 Technical Support

Zandelisib (ME-401) is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma.

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Zandelisib

Zandelisib 構造式

CAS 番号 : 1401436-95-0

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
5 mg $228 在庫あり
10 mg $365 在庫あり
25 mg $620 在庫あり
50 mg $835 在庫あり
100 mg $1145 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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製品説明

Zandelisib (ME-401) is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma[1].

IC50 & Target

IC50: 3.5 nM (p110δ)[2]

体外実験

Zandelisib (10-1000 nM, 1-24 h) sustains AKT phosphorylation (Ser473/Thr308) inhibition in SU-DHL-6 cells after wash-out[1].

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

体内実験

Zandelisib (50-100 mg/kg, p.o., once daily) significantly inhibits tumor growth in mice bearing subcutaneously inoculated SU-DHL-6 tumors[1].

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

Animal Model: SU-DHL-6 cells (1 × 107) were subcutaneously implanted into the right flank of 8-week-old male SCID mice[1]
Dosage: 50, 100 mg/kg
Administration: p.o., once daily
Result: Achieved sustained PI3Kδ inhibitory effects.
Demonstrated significant tumor growth inhibition.
Maintained effective intracellular concentration in tumor tissues.
分子量

576.68

分子式

C31H38F2N8O

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CN1CCC(C2=CC=CC=C2CC(NC3=NC(N4C5=CC=CC=C5N=C4C(F)F)=NC(N6CCOCC6)=N3)(C)C)CC1

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 : 33.33 mg/mL (57.80 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C; 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 1.7341 mL 8.6703 mL 17.3406 mL
5 mM 0.3468 mL 1.7341 mL 3.4681 mL
10 mM 0.1734 mL 0.8670 mL 1.7341 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)

Mass
=
Concentration
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Volume
×
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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.34 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
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

純度: 99.67%

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. 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 1 mM 1.7341 mL 8.6703 mL 17.3406 mL 43.3516 mL
5 mM 0.3468 mL 1.7341 mL 3.4681 mL 8.6703 mL
10 mM 0.1734 mL 0.8670 mL 1.7341 mL 4.3352 mL
15 mM 0.1156 mL 0.5780 mL 1.1560 mL 2.8901 mL
20 mM 0.0867 mL 0.4335 mL 0.8670 mL 2.1676 mL
25 mM 0.0694 mL 0.3468 mL 0.6936 mL 1.7341 mL
30 mM 0.0578 mL 0.2890 mL 0.5780 mL 1.4451 mL
40 mM 0.0434 mL 0.2168 mL 0.4335 mL 1.0838 mL
50 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8670 mL
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  • 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.

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Inquiry Information

製品名:
Zandelisib
製品番号:
HY-109198
数量:
MCE 日本正規代理店: