MASTL-IN-1
Based on 1 Customer Validation
MASTL-IN-1 is a selective and orally active MASTL inhibitor with a Ki <0.03 nM. MASTL-IN-1 inhibits phosphorylation of ENSA and inhibits proliferation in cancer cells. MASTL-IN-1 induces tumor growth inhibition and stasis in pancreatic cancer xenograft models.
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- Pureté: 99.54%
- CAS No.: 3024916-67-1
- Formule: C21H25N9
- Masse moléculaire:403.48
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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
Activité biologique
MASTL
MASTL-IN-1 (Compound 15) potently inhibits purified MASTL enzyme with a Ki of <0.03 nM[1].
MASTL-IN-1 inhibits pENSA phosphorylation in MDA-MB-231 cells with an IC50 of 1.1 nM[1].
MASTL-IN-1 inhibits pENSA phosphorylation in MiaPaca2 pancreatic cancer cells with an IC50 of 4.9 nM[1].
MASTL-IN-1 inhibits MiaPaca2 pancreatic cancer cell proliferation with an IC50 of 3.0 nM[1].
MASTL-IN-1 (100 nM) is a highly selective MASTL inhibitor, showing 420-fold selectivity over MAP4K4 and minimal off-target inhibition across a panel of 394 kinases at 100 nM[1].
MASTL-IN-1 has a Madin-Darby canine kidney cell permeability of 11.1 × 10-6 cm/sec and an apparent intrinsic clearance of 41.1 μL/min/mg in human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Bioavailability | Vdss | CL | T1/2 |
|---|---|---|---|---|---|---|
| Mice[1] | 30 mg/kg | p.o. | 96 % | 4.9 L/kg | 109 mL/min/kg | 1.2 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice (female; MiaPaca2 xenograft model)[1]
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Dosage:15 mg/kg (QD); 30 mg/kg (QD); 10 mg/kg (BID); 15 mg/kg (BID)
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Administration:p.o.; 24 days
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Result:Achieved 35% tumor growth inhibition (TGI) at day 24 with 15 mg/kg QD.
Achieved 106% TGI (tumor stasis) at day 24 with 30 mg/kg QD.
Achieved 58% TGI at day 24 with 10 mg/kg BID.
Achieved 103% TGI (tumor stasis) at day 24 with 15 mg/kg BID.
Covered MiaPaca2 IC50 for 15 hours with 15 mg/kg QD, 24 hours with 30 mg/kg QD, 21 hours with 10 mg/kg BID, and 24 hours with 15 mg/kg BID.
Covered MiaPaca2 IC90 for 9 hours with 15 mg/kg QD, 16 hours with 30 mg/kg QD, 16 hours with 10 mg/kg BID, and 19 hours with 15 mg/kg BID.
Limited average body weight loss to ≤10% across all groups, with 1 mouse in 15 mg/kg BID group and 3 mice in 30 mg/kg QD group removed due to >20% body weight loss.
Chemical Information
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CAS No. 3024916-67-1
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Appearance Solid
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Masse moléculaire 403.48
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Formule C21H25N9
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Color White to off-white
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SMILES
CN1C(C(N=C2N)=CC3=C2C=NC(NC4=NC=CC(C(CC)(N)CC)=C4)=C3)=CN=N1
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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 : 125 mg/mL (309.80 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)
Pureté et documentation
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Fiche technique (274 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 2.4784 mL | 12.3922 mL | 24.7844 mL | 61.9609 mL |
| 5 mM | 0.4957 mL | 2.4784 mL | 4.9569 mL | 12.3922 mL | |
| 10 mM | 0.2478 mL | 1.2392 mL | 2.4784 mL | 6.1961 mL | |
| 15 mM | 0.1652 mL | 0.8261 mL | 1.6523 mL | 4.1307 mL | |
| 20 mM | 0.1239 mL | 0.6196 mL | 1.2392 mL | 3.0980 mL | |
| 25 mM | 0.0991 mL | 0.4957 mL | 0.9914 mL | 2.4784 mL | |
| 30 mM | 0.0826 mL | 0.4131 mL | 0.8261 mL | 2.0654 mL | |
| 40 mM | 0.0620 mL | 0.3098 mL | 0.6196 mL | 1.5490 mL | |
| 50 mM | 0.0496 mL | 0.2478 mL | 0.4957 mL | 1.2392 mL | |
| 60 mM | 0.0413 mL | 0.2065 mL | 0.4131 mL | 1.0327 mL | |
| 80 mM | 0.0310 mL | 0.1549 mL | 0.3098 mL | 0.7745 mL | |
| 100 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6196 mL |
MASTL-IN-1 Related Classifications
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