2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
Based on 1 Customer Validation
GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 1258292-64-6
- Formula: C16H13Cl2N3O2
- Molecular Weight:350.20
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Tyk2 4.8 nM (Ki) |
JAK1 0.7 nM (Ki) |
JAK2 0.7 nM (Ki) |
JAK3 0.4 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| TF-1 | EC50 |
1.7 μM
Compound: 46
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Inhibition of JAK2 in human TF1 cells assessed as inhibition of Epo-induced STAT5 phosphorylation pretreated for 20 minutes prior to addition of cytokine by cell-based assay
Inhibition of JAK2 in human TF1 cells assessed as inhibition of Epo-induced STAT5 phosphorylation pretreated for 20 minutes prior to addition of cytokine by cell-based assay
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[PMID: 23867602] |
| TF-1 | EC50 |
2 μM
Compound: 46
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Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation pretreated for 20 minutes prior to addition of cytokine by cell-based assay
Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation pretreated for 20 minutes prior to addition of cytokine by cell-based assay
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[PMID: 23867602] |
In cell-based assays, GDC-046 demonstrates reasonable potency in blocking the IL-12 pathway (IL-12 pSTAT4 EC50=380 nM) while displaying less activity in the EPO (JAK2) pathway (EPO pSTAT5 EC50=1700 nM) and IL-6 (JAK1) pathway (IL-6 pSTAT3 EC50=2000 nM)[1].
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.
Chemical Information
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CAS No. 1258292-64-6
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Appearance Solid
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Molecular Weight 350.20
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Formula C16H13Cl2N3O2
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Color Off-white to yellow
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SMILES
O=C(NC1=CC(NC(C2CC2)=O)=NC=C1)C3=C(Cl)C=CC=C3Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 62.5 mg/mL (178.47 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). 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). 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: ≥ 2.08 mg/mL (5.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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). 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 | 2.8555 mL | 14.2776 mL | 28.5551 mL | 71.3878 mL |
| 5 mM | 0.5711 mL | 2.8555 mL | 5.7110 mL | 14.2776 mL | |
| 10 mM | 0.2856 mL | 1.4278 mL | 2.8555 mL | 7.1388 mL | |
| 15 mM | 0.1904 mL | 0.9518 mL | 1.9037 mL | 4.7592 mL | |
| 20 mM | 0.1428 mL | 0.7139 mL | 1.4278 mL | 3.5694 mL | |
| 25 mM | 0.1142 mL | 0.5711 mL | 1.1422 mL | 2.8555 mL | |
| 30 mM | 0.0952 mL | 0.4759 mL | 0.9518 mL | 2.3796 mL | |
| 40 mM | 0.0714 mL | 0.3569 mL | 0.7139 mL | 1.7847 mL | |
| 50 mM | 0.0571 mL | 0.2856 mL | 0.5711 mL | 1.4278 mL | |
| 60 mM | 0.0476 mL | 0.2380 mL | 0.4759 mL | 1.1898 mL | |
| 80 mM | 0.0357 mL | 0.1785 mL | 0.3569 mL | 0.8923 mL | |
| 100 mM | 0.0286 mL | 0.1428 mL | 0.2856 mL | 0.7139 mL |
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide Related Classifications
HY-120469 Related Classifications
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