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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- CAS. Nr.: 1428356-95-9
- Formel: C22H23N9O2
- Molecular Weight:445.48
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
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. Nr. 1428356-95-9
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Molecular Weight 445.48
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Lösungsmittel & Löslichkeit
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)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
Verweise
Complete Stock Solution Preparation Table
| 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 |