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

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

Cat. No.: HY-P4210 Purity: 99.49%
Handling Instructions 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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Custom Peptide Synthesis

Sulanemadlin

Sulanemadlin 화학구조

CAS No. : 1451199-98-6

사이즈 가격 재고 수량
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
50 mg   견적 받기  
100 mg   견적 받기  

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고객리뷰

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Sulanemadlin

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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].

In Vitro

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.

In Vivo

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.
Clinical Trial
분자량

1930.25

화학식

C95H140N20O23

CAS No.
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

선적

Room temperature in continental US; may vary elsewhere.

보관

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

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

용액&용해도
In Vitro: 

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
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.

  • 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: ≥ 2.5 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.
순도&문서

Purity: 99.49%

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 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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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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상품명:
Sulanemadlin
Cat. No.:
HY-P4210
수량:
MCE Japan Authorized Agent: