ALK5-IN-34
Based on 1 Customer Validation
ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer.
For research use only. We do not sell to patients.
- Purity: 98.21%
- CAS No.: 2785430-90-0
- Formula: C23H23N7O
- Molecular Weight:413.48
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Storage: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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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ALK5 <10 nM (IC50) |
ALK5-IN-34 (EX-11) has kinase inhibition of ALK5 with an IC50 value of ≤10 nM[1].
ALK5-IN-34 has kinase selectivity of ALK2/ALK5 with an IC50 value of ＜100 nM[1].
ALK5-IN-34 shows TGFB-RI inhibition (RD-SMAD receptor activity) with an IC50 value of ≤100 nM[1].
ALK5-IN-34 (1 μM-10 nM) inhibits the expression of TGF-β-mediated alpha-SMA in a full concentration-dependent[1].
ALK5-IN-34 (30, 300 and 3000 nM) suppresses the Treg frequency in a dose dependent manner[1].
ALK5-IN-34 (0-0.1 μM; for 6 days or 7 days) inhibits FOXL2CI34W-driven growth in KGN and COV434 cells with IC50 values of 140 nM and >10 μM, respectively[1].
ALK5-IN-34 (10, 100 and 1000 nM; 2 h) shows a dose-dependent decrease in pSmad2 in KGN cell line[1].
ALK5-IN-34 (30, 300 nM; 24 h) reverses the upregulation of gene expression in dose dependentent[1].
ALK5-IN-34 (30, 300 nM; 24 h) increases HLA class I expression in dose-dependent[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KGN and COV434 cell lines
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Concentration:0-0.1 μM
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Incubation Time:for 6 days or 7 days
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Result:Inhibited FOXL2 CI34W -driven growth.
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Cell Line:Human primary dermal fibroblasts
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Concentration:30, 300 nM
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Incubation Time:24 h
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Result:Reversed the upregulation of gene expression with TGFB stimulation.
ALK5-IN-34 (oral; 75 mg/kg; 0-24 h) shows reversely correlated between PK and tumor PD (pSMAD2 levels)[1].
ALK5-IN-34 (oral; 150 mg/kg; bid; for 22 days) increases overall survival in ES-2 ovarian cancer mouse xenograft model and can delay progression[1].
ALK5-IN-34 (p.o.; 75, 150 mg/kg; twice a day; for 21days) shows tumor growth inhibition (TGI) and increases the survival when combining with anti-PD-L1/anti-PD-1 in Syngeneic TNBC Model and in Subcutaneous Cloudman S91 melanoma model[1].
ALK5-IN-34 (oral; 300, 1000 mg/kg; bid for 5 days) has good tolerability and safety margin in Tolerability Model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549 murine xenograft model[1]
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Dosage:10, 50, 75 and 100 mg/kg
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Administration:oral gavage
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Result:Exhibited 92.5% inhibition based upon the average p-SMAD2 levels (75 mg/kg).
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Animal Model:EMT6 Syngeneic TNBC Model[1]
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Dosage:75, 150 mg/kg
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Administration:p.o., twice a day, for 21days
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Result:Resulted significantly tumor growth inhibition (TGI) by 37% at 150 mg/kg.
Result in significant tumor growth inhibition (TGI) with combination of anti-PD-LI and resulted in a significant increase in mean survival by 37%.
Resulted in significant TGI by 34% with combination of anti-PD-1 and resulted in significant increase in mean survival by 26%.
Decreased the intra-tumoral pressure.
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Animal Model:Cachexia Model[1]
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Dosage:150 mg/kg
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Administration:oral gavage, twice a day for 22 days
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Result:Showed reduction in total fluid volume and high whole limb weights.
Chemical Information
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CAS No. 2785430-90-0
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Appearance Solid
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Molecular Weight 413.48
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Formula C23H23N7O
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Color Light yellow to green yellow
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SMILES
CC1=CC=CC2=C(NC3=NC(NC4=CC=CC(N5CCOCC5)=C4)=NC=C3)C=NN=C12
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (241.85 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)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.05 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.05 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
Purity & Documentation
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Data Sheet (277 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. 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 | 2.4185 mL | 12.0925 mL | 24.1850 mL | 60.4624 mL |
| 5 mM | 0.4837 mL | 2.4185 mL | 4.8370 mL | 12.0925 mL | |
| 10 mM | 0.2418 mL | 1.2092 mL | 2.4185 mL | 6.0462 mL | |
| 15 mM | 0.1612 mL | 0.8062 mL | 1.6123 mL | 4.0308 mL | |
| 20 mM | 0.1209 mL | 0.6046 mL | 1.2092 mL | 3.0231 mL | |
| 25 mM | 0.0967 mL | 0.4837 mL | 0.9674 mL | 2.4185 mL | |
| 30 mM | 0.0806 mL | 0.4031 mL | 0.8062 mL | 2.0154 mL | |
| 40 mM | 0.0605 mL | 0.3023 mL | 0.6046 mL | 1.5116 mL | |
| 50 mM | 0.0484 mL | 0.2418 mL | 0.4837 mL | 1.2092 mL | |
| 60 mM | 0.0403 mL | 0.2015 mL | 0.4031 mL | 1.0077 mL | |
| 80 mM | 0.0302 mL | 0.1512 mL | 0.3023 mL | 0.7558 mL | |
| 100 mM | 0.0242 mL | 0.1209 mL | 0.2418 mL | 0.6046 mL |
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