MAT2A inhibitor 5
Based on 1 Customer Validation
MAT2A inhibitor 5 is an orally active, blood-brain barrier-penetrant allosteric inhibitor of MAT2A with an IC50 of 11.1 nM. MAT2A inhibitor 5 binds to the allosteric pocket of MAT2A and reduces SAM production, thereby reducing PRMT5-mediated symmetric arginine dimethylation. MAT2A inhibitor 5 selectively inhibits the proliferation of MTAP-deleted cancer cells. MAT2A inhibitor 5 inhibits tumor growth in MTAP-deleted xenograft models. MAT2A inhibitor 5 can be used for research on MTAP-deleted cancers.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 98.80%
- CAS No.: 2957874-18-7
- 화학식: C19H14ClFN4O
- 분자량:368.79
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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
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT116 MTAP-de | IC50 |
74.3 nM
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Inhibition of SDMA in HCT116 MTAP-deleted cells assessed by In-Cell Western after 96 hrs exposure.
Inhibition of SDMA in HCT116 MTAP-deleted cells assessed by In-Cell Western after 96 hrs exposure.
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acs.jmedchem.4c00552?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
| HCT116 MTAP-de | IC50 |
258.8 nM
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Antiproliferative activity against HCT116 MTAP-deleted cells assessed as viability reduction after 8 days exposure by Cell Counting-Lite 2.0 chemiluminescence assay.
Antiproliferative activity against HCT116 MTAP-deleted cells assessed as viability reduction after 8 days exposure by Cell Counting-Lite 2.0 chemiluminescence assay.
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acs.jmedchem.4c00552?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
In Vitro
MAT2A inhibitor 5 is metabolically stable in human, rat, mouse, dog, and monkey liver microsomes and hepatocytes[1].
The plasma free fractions of MAT2A inhibitor 5 in human, rat, mouse, dog, and monkey plasma are 6.2%, 5.7%, 4.4%, 7.4%, and 8.9%, respectively[1].
MAT2A inhibitor 5 exhibits high permeability in Caco-2 cells (Papp A-B 37.24 × 10-6 cm/s), with an efflux ratio as low as 0.94[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MAT2A inhibitor 5 (10-30 mg/kg; p.o.; once daily; 31 days) in female CB17 SCID mice bearing NCI-H838 MTAP-deleted subcutaneous xenograft tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, were injected subcutaneously with 5.0 × 106 HCT-116 MTAP-deleted tumor cells in 100 μL of PBS)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; once daily; 22 days
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Result:Inhibited tumor growth by 62% and 72% at 10 and 30 mg/kg once daily, respectively.
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Animal Model:CB17 SCID (female, were injected subcutaneously with 10 × 106 NCI-H838 tumor cells in200 μL of PBS and Matrigel matrix)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; once daily; 31 days
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Result:Inhibited tumor growth by 102% and 98% at 10 and 30 mg/kg once daily, respectively.
- Patient-Derived Xenograft (PDX)
- Patient-Derived Orthotopic Xenograft (PDOX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 2957874-18-7
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Appearance Solid
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분자량 368.79
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화학식 C19H14ClFN4O
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Color White to off-white
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SMILES
O=C1N(C2=CC(Cl)=C(C=C2C3=CN(N=C13)C)F)C4=CC=CN=C4C5CC5
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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 : 1.67 mg/mL (4.53 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)
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
순도&문서
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Data Sheet (297 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 | 2.7116 mL | 13.5579 mL | 27.1157 mL | 67.7893 mL |
MAT2A inhibitor 5 Related Classifications
HY-163656 Related Classifications
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