Hemiasterlin
Based on 1 Customer Validation
Hemiasterlin ((-)-Hemiasterlin) is an antimitotic marine natural product with potent anticancer effects. Hemiasterlin can be used as a cytotoxic payload (ADC Cytotoxin) in antibody-drug conjugates (ADCs).
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 157207-90-4
- Formula: C30H46N4O4
- Molecular Weight:526.71
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Pyrrolobenzodiazepines |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KB | IC50 |
76 nM
Compound: 1
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Concentration required to kill human epidermoid KBV1 cell lines containing very high levels of P-glycoprotein after 3 days of continuous exposure
Concentration required to kill human epidermoid KBV1 cell lines containing very high levels of P-glycoprotein after 3 days of continuous exposure
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[PMID: 15454219] |
| KB 3-1 | IC50 |
0.3 nM
Compound: 1
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Concentration required to kill human epidermoid KB-3-1 cell lines containing very low levels of P-glycoprotein after 3 days of continuous exposure
Concentration required to kill human epidermoid KB-3-1 cell lines containing very low levels of P-glycoprotein after 3 days of continuous exposure
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[PMID: 15454219] |
| KB 3-1 | IC50 |
1 nM
Compound: 1
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Concentration required to kill human epidermoid KB85 cell lines containing moderate levels of P-glycoprotein after 3 days of continuous exposure
Concentration required to kill human epidermoid KB85 cell lines containing moderate levels of P-glycoprotein after 3 days of continuous exposure
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[PMID: 15454219] |
| MCF7 | ED50 |
0.5 nM
Compound: hemiasterlin
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Antiproliferative activity against human MCF7 cells after 20 hrs by microculture tetrazolium assay
Antiproliferative activity against human MCF7 cells after 20 hrs by microculture tetrazolium assay
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[PMID: 26821210] |
| MCF7 | IC50 |
0.3 nM
Compound: 1
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Antimitotic activity against human MCF7 cells expressing p53 mutant by MTT assay
Antimitotic activity against human MCF7 cells expressing p53 mutant by MTT assay
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[PMID: 12608848] |
| MCF7 | IC50 |
0.3 nM
Compound: 1
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Cytotoxicity activity against human MCF7 cells expressing p53 mutant by MTT assay
Cytotoxicity activity against human MCF7 cells expressing p53 mutant by MTT assay
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[PMID: 12608848] |
Chemical Information
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CAS No. 157207-90-4
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Appearance Solid
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Molecular Weight 526.71
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Formula C30H46N4O4
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Color White to off-white
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SMILES
OC(/C(C)=C/[C@H](C(C)C)N(C)C([C@H](C(C)(C)C)NC([C@@H](NC)C(C)(C1=CN(C)C2=CC=CC=C12)C)=O)=O)=O
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Synonyms
(-)-Hemiasterlin; Milnamide B
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (189.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). 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 (protect from light). 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 (4.75 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 (4.75 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 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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 (protect from light)
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
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Data Sheet (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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 (protect from light). 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 | 1.8986 mL | 9.4929 mL | 18.9858 mL | 47.4644 mL |
| 5 mM | 0.3797 mL | 1.8986 mL | 3.7972 mL | 9.4929 mL | |
| 10 mM | 0.1899 mL | 0.9493 mL | 1.8986 mL | 4.7464 mL | |
| 15 mM | 0.1266 mL | 0.6329 mL | 1.2657 mL | 3.1643 mL | |
| 20 mM | 0.0949 mL | 0.4746 mL | 0.9493 mL | 2.3732 mL | |
| 25 mM | 0.0759 mL | 0.3797 mL | 0.7594 mL | 1.8986 mL | |
| 30 mM | 0.0633 mL | 0.3164 mL | 0.6329 mL | 1.5821 mL | |
| 40 mM | 0.0475 mL | 0.2373 mL | 0.4746 mL | 1.1866 mL | |
| 50 mM | 0.0380 mL | 0.1899 mL | 0.3797 mL | 0.9493 mL | |
| 60 mM | 0.0316 mL | 0.1582 mL | 0.3164 mL | 0.7911 mL | |
| 80 mM | 0.0237 mL | 0.1187 mL | 0.2373 mL | 0.5933 mL | |
| 100 mM | 0.0190 mL | 0.0949 mL | 0.1899 mL | 0.4746 mL |
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