THRX-144644
Based on 1 Customer Validation
THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition.
For research use only. We do not sell to patients.
- Purity: 99.43%
- CAS No.: 2442519-59-5
- Formula: C26H28ClF2N7
- Molecular Weight:512.00
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Biological Activity
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ALK5 0.14 nM (IC50) |
THRX-144644 (1-10000 nM; 1 h) inhibits ALK5 with an IC50 value of 23 nM in human BEAS2B cell line.
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:Sprague Dawley rats[1]
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Dosage:2, 10, and 60 mg/kg
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Administration:Inhalation: nebulizer, daily, for 14 days
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Result:Had the L:P ratio (AUC) was 0.44.
Had lung-to-plasma ratios ranged from 100- to 1200-fold in rats across dose level.
Had lung trough (24 h) concentrations in rats ranged from 3- to 17-fold above the PCLS IC50 across tolerated doses.
Chemical Information
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CAS No. 2442519-59-5
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Appearance Solid
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Molecular Weight 512.00
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Formula C26H28ClF2N7
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Color White to yellow
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SMILES
FC1=CC(F)=C(C2=NNC=C2C3=NC4=C(C=C3)N=CC(NCCN5CCN(C(C)C)CC5)=C4)C=C1Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 50 mg/mL (97.66 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, stored under nitrogen). 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, stored under nitrogen). 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)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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, stored under nitrogen). 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 | 1.9531 mL | 9.7656 mL | 19.5312 mL | 48.8281 mL |
| 5 mM | 0.3906 mL | 1.9531 mL | 3.9062 mL | 9.7656 mL | |
| 10 mM | 0.1953 mL | 0.9766 mL | 1.9531 mL | 4.8828 mL | |
| 15 mM | 0.1302 mL | 0.6510 mL | 1.3021 mL | 3.2552 mL | |
| 20 mM | 0.0977 mL | 0.4883 mL | 0.9766 mL | 2.4414 mL | |
| 25 mM | 0.0781 mL | 0.3906 mL | 0.7812 mL | 1.9531 mL | |
| 30 mM | 0.0651 mL | 0.3255 mL | 0.6510 mL | 1.6276 mL | |
| 40 mM | 0.0488 mL | 0.2441 mL | 0.4883 mL | 1.2207 mL | |
| 50 mM | 0.0391 mL | 0.1953 mL | 0.3906 mL | 0.9766 mL | |
| 60 mM | 0.0326 mL | 0.1628 mL | 0.3255 mL | 0.8138 mL | |
| 80 mM | 0.0244 mL | 0.1221 mL | 0.2441 mL | 0.6104 mL |