1. Apoptosis
  2. MDM-2/p53
  3. Sulanemadlin

Sulanemadlin  (Synonyms: ALRN-6924; MP-4897)

製品番号: HY-P4210 純度: 99.49%
COA 取扱説明書 Technical Support

Sulanemadlin (ALRN-6924) is a potent and cell-permeating p53-based peptidomimetic macrocycles. Sulanemadlin is a inhibitor of the p53-MDM2, p53-MDMX, or both p53 and MDM2 and MDMX protein-protein interactions. Sulanemadlin can be used for cancers research.

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カスタムペプチド

Sulanemadlin

Sulanemadlin 構造式

CAS 番号 : 1451199-98-6

容量 価格(税別) 在庫状況 数量
1 mg $350 在庫あり
5 mg $950 在庫あり
10 mg $1500 在庫あり
50 mg   お問い合わせ  
100 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 1 publication(s) in Google Scholar

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製品説明

Sulanemadlin (ALRN-6924) is a potent and cell-permeating p53-based peptidomimetic macrocycles. Sulanemadlin is a inhibitor of the p53-MDM2, p53-MDMX, or both p53 and MDM2 and MDMX protein-protein interactions. Sulanemadlin can be used for cancers research[1].

Cellular Effect
Cell Line Type Value Description References
SJSA-1 EC50
0.3 μM
Compound: ALRN-6924
Cytotoxicity against human SJSA-1 cells incubated for 72 hrs in presence of 10% FBS by MTT assay
Cytotoxicity against human SJSA-1 cells incubated for 72 hrs in presence of 10% FBS by MTT assay
[PMID: 37439511]
体外実験

Sulanemadlin (0-10 μM, 24 h) induces reversible, dose-dependent cell cycle arrest in CD34+ human bone marrow cells, and protects cells from Topotecan (HY-13768)-induced DNA damage[2].

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

体内実験

Sulanemadlin (5-20 mg/kg, i.v.) shows antitumor activity in multiple TP53-WT subcutaneous mouse xenograft models[1].
Sulanemadlin (2.4 mg/kg, daily with for 5 days, 24 h prior to daily 1.5 mg/kg Topotecan) protects mice against Topotecan-induced neutropenia and gastrointestinal toxicity in mice, without diminishing Topotecan antitumor activity in TP53-mutant cancer models[1].
PK properties of Sulanemadlin.

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

Species Dose (mg/kg) Cmax (μg/mL) AUCall (μg·h/mL) T1/2 (h) CL (mL/h/kg)
Mouse 5 67.8 450 2.2 11
Rat 5 95.9 223 2.0 24
Monkey 5 137 914 4.9 5.9
Animal Model: MCF-7 breast cancer, SJSA1 osteosarcoma, and patient-derived melanoma xenograft models[1]
Dosage: 5-20 mg/kg
Administration: i.v.
Result: Inhibited tumor growth.
Induced accumulation of the p53 protein and increased p21 protein expression (maximum effect at 16 h post-dose).
Decreased BrdU level.
臨床実験
分子量

1930.25

分子式

C95H140N20O23

CAS 番号
Appearance

Solid

Color

White to off-white

Sequence

Ac-Leu-Thr-Phe-R8-Glu-Tyr-Trp-Ala-Gln-Leu-S5-Ala-Ala-Ala-Ala-Ala-{dAla}-NH2

Sequence Shortening

Ac-LTF-R8-EYWAQL-S5-AAAAA-{dAla}-NH2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

polypeptide, sealed storage, away from moisture and light, under nitrogen

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

溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (51.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.5181 mL 2.5903 mL 5.1807 mL
5 mM 0.1036 mL 0.5181 mL 1.0361 mL
10 mM 0.0518 mL 0.2590 mL 0.5181 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 and light, under nitrogen). 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)

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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)

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体積 (開始)

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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 (1.30 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (1.30 mM); Suspended solution

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

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

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: 99.49%

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 and light, under nitrogen). 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 0.5181 mL 2.5903 mL 5.1807 mL 12.9517 mL
5 mM 0.1036 mL 0.5181 mL 1.0361 mL 2.5903 mL
10 mM 0.0518 mL 0.2590 mL 0.5181 mL 1.2952 mL
15 mM 0.0345 mL 0.1727 mL 0.3454 mL 0.8634 mL
20 mM 0.0259 mL 0.1295 mL 0.2590 mL 0.6476 mL
25 mM 0.0207 mL 0.1036 mL 0.2072 mL 0.5181 mL
30 mM 0.0173 mL 0.0863 mL 0.1727 mL 0.4317 mL
40 mM 0.0130 mL 0.0648 mL 0.1295 mL 0.3238 mL
50 mM 0.0104 mL 0.0518 mL 0.1036 mL 0.2590 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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製品名:
Sulanemadlin
製品番号:
HY-P4210
数量:
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