CH5138303
Based on 1 Customer Validation
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model.
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- Purity: 99.04%
- CAS No.: 959763-06-5
- 화학식: C19H18ClN5O2S
- 분자량:415.90
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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HSP90α 0.52 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.098 μM
Compound: 16l, CH5138303
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Cytotoxicity against human HCT116 cells after 4 days by CCk-8 assay
Cytotoxicity against human HCT116 cells after 4 days by CCk-8 assay
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[PMID: 24369839] |
| NCI-N87 | ED50 |
3.9 mg/kg
Compound: 16l, CH5138303
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Antitumor activity against human NCI-N87 cells xenografted in po dosed BALB/c nu/nu mouse assessed as tumor growth inhibition administered qd for 11 days
Antitumor activity against human NCI-N87 cells xenografted in po dosed BALB/c nu/nu mouse assessed as tumor growth inhibition administered qd for 11 days
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[PMID: 24369839] |
| NCI-N87 | IC50 |
0.066 μM
Compound: 16l, CH5138303
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Cytotoxicity against human NCI-N87 cells after 4 days by CCk-8 assay
Cytotoxicity against human NCI-N87 cells after 4 days by CCk-8 assay
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[PMID: 24369839] |
When used in combination with FLC, CH5138303 shows antifungal activitiy against azole-resistant C. albicans, with a FICI (fractional inhibitory concentration index) of 0.500[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.
Chemical Information
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CAS No. 959763-06-5
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Appearance Solid
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분자량 415.90
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화학식 C19H18ClN5O2S
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Color White to yellow
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SMILES
O=C(N)CCCSC1=NC(N)=NC(C2=C(Cl)C=C3C4=C2C=CC=C4COC3)=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
DMSO : 100 mg/mL (240.44 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.01 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.
순도&문서
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 2.4044 mL | 12.0221 mL | 24.0442 mL | 60.1106 mL |
| 5 mM | 0.4809 mL | 2.4044 mL | 4.8088 mL | 12.0221 mL | |
| 10 mM | 0.2404 mL | 1.2022 mL | 2.4044 mL | 6.0111 mL | |
| 15 mM | 0.1603 mL | 0.8015 mL | 1.6029 mL | 4.0074 mL | |
| 20 mM | 0.1202 mL | 0.6011 mL | 1.2022 mL | 3.0055 mL | |
| 25 mM | 0.0962 mL | 0.4809 mL | 0.9618 mL | 2.4044 mL | |
| 30 mM | 0.0801 mL | 0.4007 mL | 0.8015 mL | 2.0037 mL | |
| 40 mM | 0.0601 mL | 0.3006 mL | 0.6011 mL | 1.5028 mL | |
| 50 mM | 0.0481 mL | 0.2404 mL | 0.4809 mL | 1.2022 mL | |
| 60 mM | 0.0401 mL | 0.2004 mL | 0.4007 mL | 1.0018 mL | |
| 80 mM | 0.0301 mL | 0.1503 mL | 0.3006 mL | 0.7514 mL | |
| 100 mM | 0.0240 mL | 0.1202 mL | 0.2404 mL | 0.6011 mL |
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