Hypothemycin
Based on 1 Customer Validation
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.
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- Pureté: 98.0%
- CAS No.: 76958-67-3
- Formule: C19H22O8
- Masse moléculaire:378.37
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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VEGFR2 10 nM (Ki) |
VEGFR1 70 nM (Ki) |
MEK1 17 nM (Ki) |
MEK2 38 nM (Ki) |
FLT-3 90 nM (Ki) |
PDGFRα 1.5 μM (Ki) |
PDGFRβ 900 nM (Ki) |
ERK1 8.4 μM (Ki) |
ERK2 2.4 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1 μM
Compound: 17
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Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
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[PMID: 28749671] |
| COLO-829 | IC50 |
0.15 μM
Compound: hypothemycin
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Cytotoxicity against human COLO829 cells
Cytotoxicity against human COLO829 cells
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[PMID: 17067161] |
| HeLa | IC50 |
1 μM
Compound: 17
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Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
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[PMID: 28749671] |
| HT-29 | IC50 |
5.9 μM
Compound: hypothemycin
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Cytotoxicity against human HT-29 cells
Cytotoxicity against human HT-29 cells
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[PMID: 17067161] |
| Jurkat | IC50 |
>1 μM
Compound: HY
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Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 30742435] |
| MCF7 | IC50 |
16.3 μM
Compound: 7
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Cytotoxicity against human MCF7 cells after 72 hrs by MTS assay
Cytotoxicity against human MCF7 cells after 72 hrs by MTS assay
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[PMID: 21513293] |
| MCF7 | IC50 |
3.3 μM
Compound: 17
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Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
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[PMID: 28749671] |
| MDA-MB-435 | IC50 |
1.9 μM
Compound: HPO
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Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-blue cell viability assay
Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-blue cell viability assay
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[PMID: 35834411] |
| MV4-11 | IC50 |
15 nM
Compound: HY
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Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay
Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay
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[PMID: 30742435] |
| NCI-H460 | IC50 |
4.3 μM
Compound: 7
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Cytotoxicity against human H460 cells after 72 hrs by MTS assay
Cytotoxicity against human H460 cells after 72 hrs by MTS assay
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[PMID: 21513293] |
| OVCAR-3 | IC50 |
2.6 μM
Compound: HPO
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Cytotoxicity against human OVCAR-3 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-blue cell viability assay
Cytotoxicity against human OVCAR-3 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-blue cell viability assay
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[PMID: 35834411] |
| SF-268 | IC50 |
12.7 μM
Compound: 7
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Cytotoxicity against human SF268 cells after 72 hrs by MTS assay
Cytotoxicity against human SF268 cells after 72 hrs by MTS assay
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[PMID: 21513293] |
| SK-OV-3 | IC50 |
0.07 μM
Compound: hypothemycin
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Cytotoxicity against human SKOV3 cells
Cytotoxicity against human SKOV3 cells
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[PMID: 17067161] |
| THP-1 | IC50 |
>1 μM
Compound: HY
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Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 30742435] |
Hypothemycin inhibits eosinophilic EOL1 cell carrying mutations in FIP1L1-PDGFRα, acute myeloid leukemia MV-4-11 cell carrying mutations in FLT3-ITD, melanoma COLO829 cell carrying mutations in BRAF V600E, HUVEC cell carrying mutations in VEGFR, mastocytoma P815 cell carrying mutations in c-KIT D814Y, NSCLC A459 cell carrying mutations in KRAS, and ovarian SKOV-3 cell carrying mutations in HER2 with IC50s of 0.4 nM, 6 nM, 50 nM, 70 nM, 370 nM, 6.0 μM, and 7.0 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult female Balb/c mice (weighing 18–22 g) infected with T. brucei[1]
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Dosage:10 mg/kg
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Administration:Administered once daily via intraperitoneal injection for 7 days.
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Result:Showed a dose-dependent reduction in parasitemia in infected mice.
Prolonged survival of infected mice over 30 days, with a cure rate of 33%.
Chemical Information
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CAS No. 76958-67-3
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Appearance Solid
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Masse moléculaire 378.37
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Formule C19H22O8
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Color White to off-white
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SMILES
COC1=CC(O)=C(C(O[C@@H](C)C/C=C\C2=O)=O)C([C@@H](O3)[C@@]3([H])C[C@H](O)[C@@H]2O)=C1
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Structure Classification
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Initial Source
Hypomyces trichothecoides
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (264.29 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. 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. 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 (6.61 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 (6.61 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.
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.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Schirmer A, et al. Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides. Proc Natl Acad Sci U S A. 2006 Mar 14;103(11):4234-9. [Content Brief]
[2]. Nishino M, et al. Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei. Elife. 2013 Jul 9;2:e00712. [Content Brief]
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 | 2.6429 mL | 13.2146 mL | 26.4292 mL | 66.0729 mL |
| 5 mM | 0.5286 mL | 2.6429 mL | 5.2858 mL | 13.2146 mL | |
| 10 mM | 0.2643 mL | 1.3215 mL | 2.6429 mL | 6.6073 mL | |
| 15 mM | 0.1762 mL | 0.8810 mL | 1.7619 mL | 4.4049 mL | |
| 20 mM | 0.1321 mL | 0.6607 mL | 1.3215 mL | 3.3036 mL | |
| 25 mM | 0.1057 mL | 0.5286 mL | 1.0572 mL | 2.6429 mL | |
| 30 mM | 0.0881 mL | 0.4405 mL | 0.8810 mL | 2.2024 mL | |
| 40 mM | 0.0661 mL | 0.3304 mL | 0.6607 mL | 1.6518 mL | |
| 50 mM | 0.0529 mL | 0.2643 mL | 0.5286 mL | 1.3215 mL | |
| 60 mM | 0.0440 mL | 0.2202 mL | 0.4405 mL | 1.1012 mL | |
| 80 mM | 0.0330 mL | 0.1652 mL | 0.3304 mL | 0.8259 mL | |
| 100 mM | 0.0264 mL | 0.1321 mL | 0.2643 mL | 0.6607 mL |
Hypothemycin Related Classifications
HY-107417 Related Classifications
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