ISM5939
Based on 1 Customer Validation
ISM5939 is an orally active and selective ENPP1 inhibitor with an IC50 of 0.63 nM for 2,3-cGAMP degradation and 9.28 nM for ATP hydrolysis. ISM5939 has antitumor activity.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.79%
- CAS No.: 2965301-60-2
- 화학식: C20H18FN5O3S
- 분자량:427.45
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보관:Powder -20°C, 3 years , 4°C, 2 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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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
Parmacokinetics
| Species | Dose | Route | Bioavailability | Clearance (CL) | Vss |
|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 32 % | 14 mL/min/kg | 0.53 L/kg |
| Mice[1] | 5 mg/kg | p.o. | 32 % | 14 mL/min/kg | 0.53 L/kg |
| Mice[1] | 1 mg/kg | i.v. | 49 % | 14 mL/min/kg | 1.1 L/kg |
| Mice[1] | 5 mg/kg | p.o. | 49 % | 14 mL/min/kg | 1.1 L/kg |
| Mice[1] | 0.5 mg/kg | i.v. | 45 % | 2.0 mL/min/kg | 0.63 L/kg |
| Mice[1] | 1 mg/kg | p.o. | 45 % | 2.0 mL/min/kg | 0.63 L/kg |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2965301-60-2
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Appearance Solid
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분자량 427.45
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화학식 C20H18FN5O3S
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Color White to off-white
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SMILES
COC1=C(C2=CC=CC=C2)C3=C(C=N1)N=C(C)N3CC4=C(F)C=C(S(N)(=O)=O)C=N4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 200 mg/mL (467.89 mM; Need ultrasonic and warming; 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)
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
순도&문서
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Data Sheet (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 2.3395 mL | 11.6973 mL | 23.3945 mL | 58.4864 mL |
| 5 mM | 0.4679 mL | 2.3395 mL | 4.6789 mL | 11.6973 mL | |
| 10 mM | 0.2339 mL | 1.1697 mL | 2.3395 mL | 5.8486 mL | |
| 15 mM | 0.1560 mL | 0.7798 mL | 1.5596 mL | 3.8991 mL | |
| 20 mM | 0.1170 mL | 0.5849 mL | 1.1697 mL | 2.9243 mL | |
| 25 mM | 0.0936 mL | 0.4679 mL | 0.9358 mL | 2.3395 mL | |
| 30 mM | 0.0780 mL | 0.3899 mL | 0.7798 mL | 1.9495 mL | |
| 40 mM | 0.0585 mL | 0.2924 mL | 0.5849 mL | 1.4622 mL | |
| 50 mM | 0.0468 mL | 0.2339 mL | 0.4679 mL | 1.1697 mL | |
| 60 mM | 0.0390 mL | 0.1950 mL | 0.3899 mL | 0.9748 mL | |
| 80 mM | 0.0292 mL | 0.1462 mL | 0.2924 mL | 0.7311 mL | |
| 100 mM | 0.0234 mL | 0.1170 mL | 0.2339 mL | 0.5849 mL |
ISM5939 Related Classifications
HY-176708 Related Classifications
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