CHD1Li 6.11
Based on 1 Customer Validation
CHD1Li 6.11 is a potent and orally active Chromodomain Helicase DNA Binding Protein 1 Like (CHD1L) (oncogenic gene) inhibitor (IC50 = 3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 can inhibit EMT, induce mesenchymal-epithelial transition (reverse EMT) and promote apoptosis in tumor organoid models. CHD1Li 6.11 can be used for the research of cancer, such as colorectal cancer.
For research use only. We do not sell to patients.
- Purity: 99.54%
- CAS No.: 2716890-91-2
- Formula: C21H22BrN5OS
- Molecular Weight:472.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All DNA/RNA Synthesis Isoforms
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Biological Activity
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Helicase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.8 μM
Compound: 6.11
|
Inhibition of cell stemness in human HCT-116 M-phenotype cells assessed as reduction in colony formation
Inhibition of cell stemness in human HCT-116 M-phenotype cells assessed as reduction in colony formation
|
[PMID: 35192363] |
| HCT-116 | IC50 |
4.3 μM
Compound: 6.11
|
Cytotoxicity against human HCT-116 M-phenotype tumor organoid assessed as reduction in cell viability incubated for 72 hrs by CellTiter Glo assay
Cytotoxicity against human HCT-116 M-phenotype tumor organoid assessed as reduction in cell viability incubated for 72 hrs by CellTiter Glo assay
|
[PMID: 35192363] |
| HCT-116 | IC50 |
5 μM
Compound: 6.11
|
Induction of mesenchymal-epithelial transition in human HCT-116 M-phenotype tumor organoid assessed as downregulation of vimentin expression by fluorescence analysis
Induction of mesenchymal-epithelial transition in human HCT-116 M-phenotype tumor organoid assessed as downregulation of vimentin expression by fluorescence analysis
|
[PMID: 35192363] |
| SW-620 | IC50 |
1.6 μM
Compound: 6.11
|
Inhibition of cell stemness in human SW-620 M-phenotype cells assessed as reduction in colony formation
Inhibition of cell stemness in human SW-620 M-phenotype cells assessed as reduction in colony formation
|
[PMID: 35192363] |
| SW-620 | IC50 |
2.6 μM
Compound: 6.11
|
Cytotoxicity against human SW-620 M-phenotype tumor organoid assessed as reduction in cell viability incubated for 72 hrs by CellTiter Glo assay
Cytotoxicity against human SW-620 M-phenotype tumor organoid assessed as reduction in cell viability incubated for 72 hrs by CellTiter Glo assay
|
[PMID: 35192363] |
| SW-620 | IC50 |
2.6 μM
Compound: 6.11
|
Cytotoxicity against human SW-620 tumor organoid assessed as reduction in cell viability incubated for 72 hrs by CellTiter Glo assay
Cytotoxicity against human SW-620 tumor organoid assessed as reduction in cell viability incubated for 72 hrs by CellTiter Glo assay
|
[PMID: 35192363] |
| SW-620 | IC50 |
3.3 μM
Compound: 6.11
|
Induction of mesenchymal-epithelial transition in human SW-620 M-phenotype tumor organoid assessed as downregulation of vimentin expression by fluorescence analysis
Induction of mesenchymal-epithelial transition in human SW-620 M-phenotype tumor organoid assessed as downregulation of vimentin expression by fluorescence analysis
|
[PMID: 35192363] |
CHD1Li 6.11 shows an IC50 of 2.6 μM against SW620 tumor organoid[1].
CHD1Li 6.11 (1-100 μM, 24 h) reduces TCF-transcription in M-Phenotype SW620 and HCT116 cells[1].
CHD1Li 6.11 (1-100 μM, 72 h) reduces viabilities in M-Phenotype SW620 and HCT116 cells[1].
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:Athymic nude mouse xenografts baring SW620 isolated M-Phenotype flank tumors[1]
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Dosage:75 and 125 mg/kg
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Administration:Orally administration, 5 times a week for 28 days
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Result:Reduced tumor volume.
Had no abnormal observations associated with gross toxicity.
Chemical Information
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CAS No. 2716890-91-2
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Appearance Solid
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Molecular Weight 472.40
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Formula C21H22BrN5OS
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Color Off-white to gray
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SMILES
O=C(NC1=CC=C(NC2=NC(N3CCCC3)=NC(C)=C2)C=C1)CC4=CC(Br)=CS4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (211.69 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 (5.29 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.
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.
Purity & Documentation
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Data Sheet (271 KB)
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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)
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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. 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 | 2.1169 mL | 10.5843 mL | 21.1685 mL | 52.9213 mL |
| 5 mM | 0.4234 mL | 2.1169 mL | 4.2337 mL | 10.5843 mL | |
| 10 mM | 0.2117 mL | 1.0584 mL | 2.1169 mL | 5.2921 mL | |
| 15 mM | 0.1411 mL | 0.7056 mL | 1.4112 mL | 3.5281 mL | |
| 20 mM | 0.1058 mL | 0.5292 mL | 1.0584 mL | 2.6461 mL | |
| 25 mM | 0.0847 mL | 0.4234 mL | 0.8467 mL | 2.1169 mL | |
| 30 mM | 0.0706 mL | 0.3528 mL | 0.7056 mL | 1.7640 mL | |
| 40 mM | 0.0529 mL | 0.2646 mL | 0.5292 mL | 1.3230 mL | |
| 50 mM | 0.0423 mL | 0.2117 mL | 0.4234 mL | 1.0584 mL | |
| 60 mM | 0.0353 mL | 0.1764 mL | 0.3528 mL | 0.8820 mL | |
| 80 mM | 0.0265 mL | 0.1323 mL | 0.2646 mL | 0.6615 mL | |
| 100 mM | 0.0212 mL | 0.1058 mL | 0.2117 mL | 0.5292 mL |