CIDD-8633
Based on 1 Customer Validation
CIDD-8633 is a potent DDR2 inhibitor with an IC50 of 6.105 μM. CIDD-8633 inhibits cell migration and halts the cell cycle and induces apoptosis, significantly suppressing pancreatic ductal adenocarcinoma (PDAC) tumor growth. CIDD-8633 can be used for the study of pancreatic cancer such as PDAC.
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- Pureté : 99.42%
- CAS No.: 1428356-95-9
- Formule: C22H23N9O2
- Masse moléculaire:445.48
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
DDR2 6.105 μM (IC50) |
Caspase 3 |
IL-6 |
In Vitro
CIDD-8633 (4-5.5 μM, 7-10 days) inhibits the long-term clonal formation ability of AsPC1 and MIA-PaCa-2 cells[1].
CIDD-8633 (4-6 μM, 72 h) significantly reduces the levels of phosphorylated-DDR2 and its downstream effector phospho-ERK in AsPC1 and MIA-PaCa-2 cells[1].
CIDD-8633 (1.5 μM, 48 h) inhibits the nuclear translocation of the DDR2-ERK signaling pathway and blocks the proliferative signals in AsPC1 and MIA-PaCa-2 cells[1].
CIDD-8633 (0.1-10 μM, 72 h) significantly reduces the proliferation of MIA-PaCa-2 cells and AsPC-1 with IC25s of 4.0 and 5.5 μM, respectively[1].
CIDD-8633 (4 μM, 16 h) reduces the migration ability of MIA PaCa-2 cells by inhibiting DDR2[1].
CIDD-8633 (4-6 μM, 72 h) inhibits the cell cycle progression by blocking the G1/S phase in AsPC1 and MIA-PaCa-2 cells
CIDD-8633 (4-6 μM, 72 h) induces apoptosis in AsPC1 and MIA-PaCa-2 cells by activating caspase-3[1].
CIDD-8633 (6 μM, 48 h) upregulates the genes including CDKN1A, DDIT3, IL-1β, PMAIP1, and CASP4 in AsPC1 and MIA-PaCa-2 cells[1].
CIDD-8633 (4-10 μM, 72 h) significantly reduces the levels of p-DDR2 and p-ERK, and increases the level of cleaved caspase-3 in AsPC1 and MIA-PaCa-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AsPC1 and MIA-PaCa-2 cells
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Concentration:1.5 μM
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Incubation Time:48 h
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Result:Localized the phospho-ERK was predominantly in the nucleus of cells.
Resulted in more cytoplasmic localization of phospho-ERK and a marked decrease in its intensity.
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Cell Line:GC68, AsPC1, MIA-PaCa-2, Panc02 and KPC cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:72 h
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Result:Exhibited IC50s of 6.088, 6.284, 5.025, 4.926 and 10.05 μM, respectively.
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Cell Line:AsPC1 and MIA-PaCa-2 cells
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Concentration:6 μM
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Incubation Time:48 h
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Result:Increased the levels of CDKN1A, DDIT3, IL-1β, PMAIP1 and CASP4.
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Cell Line:AsPC1 and MIA-PaCa-2 cells
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Concentration:4 and 6 μM
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Incubation Time:72 h
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Result:Increased the proportion of apoptotic cells by 2 to 3 times.
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Cell Line:AsPC1 and MIA-PaCa-2 cells
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Concentration:4 and 6 μM
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Incubation Time:72 h
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Result:Increased the proportion of G1 phase cells by 20-30%.
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Cell Line:AsPC1 and MIA-PaCa-2 cells
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Concentration:6 μM
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Incubation Time:48 h
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Result:Increased the levels of CDKN1A, DDIT3, IL-1β, PMAIP1 and CASP4.
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Cell Line:AsPC1 and MIA-PaCa-2 cells
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Concentration:4 and 6 μM
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Incubation Time:72 h
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Result:Decreased the levels of p-DDR2 and p-ERK.
Increased the level of cleaved caspase-3.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MIA PaCa-2 induced PDAC model established in NOD/SCID mice[1]
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Dosage:40 mg/kg
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Administration:Intraperitoneal injection (i.p.), twice a week for 28 days
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Result:Significant decreased the tumor weight and volume. Decreased the levels of p-DDR2 and p-ERK.
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Animal Model:Pan02 induced PDAC model established in C57BL/6J mice[1]
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Dosage:40 mg/kg
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Administration:Intraperitoneal injection (i.p.), twice a week for 28 days
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Result:Delayed the tumor growth.
Decreased the levels of p-DDR2 and p-ERK.
- Scratch/Wound-Healing Migration Assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- Cell migration
- BrdU Incorporation Assay
- Neural Crest/Neuronal Cell Migration Explant Assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Zigmond Chamber Chemotaxis Assay
- Under-Agarose Cell Migration Assay
- Transwell/Boyden Chamber Migration Assay
- Patient-Derived Xenograft (PDX)
- 3D Collagen/Hydrogel Matrix Migration Assay
- Apoptosis Solutions
- Subcutaneous Cell-Line-Derived Xenograft
- Cell-Exclusion Zone Migration Assay
- Dunn/Insall Chamber Chemotaxis Assay
- Orthotopic Cell-Line Xenograft
Chemical Information
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CAS No. 1428356-95-9
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Appearance Solid
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Masse moléculaire 445.48
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Formule C22H23N9O2
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SMILES
O=C(NC1=CC=C(NC2=NC(NCC)=NC(C)=C2)C=C1)COC(C=C3)=NN=C3N4C=CC=N4
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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
In Vitro:
DMSO : 50 mg/mL (112.24 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
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2448 mL | 11.2238 mL | 22.4477 mL | 56.1192 mL |
| 5 mM | 0.4490 mL | 2.2448 mL | 4.4895 mL | 11.2238 mL | |
| 10 mM | 0.2245 mL | 1.1224 mL | 2.2448 mL | 5.6119 mL | |
| 15 mM | 0.1497 mL | 0.7483 mL | 1.4965 mL | 3.7413 mL | |
| 20 mM | 0.1122 mL | 0.5612 mL | 1.1224 mL | 2.8060 mL | |
| 25 mM | 0.0898 mL | 0.4490 mL | 0.8979 mL | 2.2448 mL | |
| 30 mM | 0.0748 mL | 0.3741 mL | 0.7483 mL | 1.8706 mL | |
| 40 mM | 0.0561 mL | 0.2806 mL | 0.5612 mL | 1.4030 mL | |
| 50 mM | 0.0449 mL | 0.2245 mL | 0.4490 mL | 1.1224 mL | |
| 60 mM | 0.0374 mL | 0.1871 mL | 0.3741 mL | 0.9353 mL | |
| 80 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7015 mL | |
| 100 mM | 0.0224 mL | 0.1122 mL | 0.2245 mL | 0.5612 mL |
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