Sulanemadlin
Based on 2 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.49%
- CAS No.: 1451199-98-6
- Formula: C95H140N20O23
- Molecular Weight:1930.25
-
Storage:
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)
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Sulanemadlin
More
Biological Activity
|
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] |
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.
| 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 |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1451199-98-6
-
Appearance Solid
-
Molecular Weight 1930.25
-
Formula C95H140N20O23
-
Color White to off-white
-
Synonyms
ALRN-6924; MP-4897
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
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)
Publications (2)
-
Journal Impact Factor
-
Most Recent
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Purity & Documentation
-
Data Sheet (276 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
Handling Instructions (2659 KB)
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 |
Powered by Bioz