2. Protein Tyrosine Kinase/RTK Apoptosis Immunology/Inflammation
  3. Discoidin Domain Receptor Apoptosis Caspase Interleukin Related
  4. CIDD-8633

CIDD-8633 is a potent DDR2 inhibitor with an IC50 of 6.105 μM. CIDD-8633 significantly reduces the proliferation of MIA-PaCa-2 cells and AsPC-1 with IC25s of 4.0 and 5.5 μM, respectively. 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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CIDD-8633 Chemical Structure

CIDD-8633 Chemical Structure

CAS No. : 1428356-95-9

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CIDD-8633 Related Antibodies

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DDR1 DDR2

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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Description

CIDD-8633 is a potent DDR2 inhibitor with an IC50 of 6.105 μM. CIDD-8633 significantly reduces the proliferation of MIA-PaCa-2 cells and AsPC-1 with IC25s of 4.0 and 5.5 μM, respectively. 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[1].

IC50 & Target[1]

DDR2

6.105 μM (IC50)

Caspase 3

 

IL-6

 

In Vitro

CIDD-8633 (40°C-64°C) increases the stability of the DDR2 protein in AsPC-1, MIA, PaCa-2 and KPC cells[1].
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 reduced 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) reduces the proliferation of PDAC cells in a dose-dependent manner[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[1].
CIDD-8633 (4-6 μM, 72 h) by activating caspase-3 to induce apoptosis in AsPC1 and MIA-PaCa-2 cells[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.

CIDD-8633 Related Antibodies

Immunofluorescence[1]

Cell Line: AsPC1 and MIA-PaCa-2 cells
Concentration: 1.5 μM
Incubation Time: 48 h
Result: The phospho-ERK was predominantly localized in the nucleus of cells.
Resulted in more cytoplasmic localization of phospho-ERK and a marked decrease in its intensity.

Cell Viability Assay[1]

Cell Line: GC68, AsPC1, MIA-PaCa-2, Panc02 and KPC cells
Concentration: 0.1, 1 and 10 μM
Incubation Time: 72 h
Result: Exhibited IC50s of 6.088, 6.284, 5.025, 4.926 and 10.05 μM, respectively.

Cell Migration Assay [1]

Cell Line: AsPC1 and MIA-PaCa-2 cells
Concentration: 6 μM
Incubation Time: 48 h
Result: Increased the levels of CDKN1A, DDIT3, IL-1β, PMAIP1 and CASP4.

Apoptosis Analysis[1]

Cell Line: AsPC1 and MIA-PaCa-2 cells
Concentration: 4 and 6 μM
Incubation Time: 72 h
Result: The proportion of apoptotic cells increased by 2 to 3 times.

Cell Cycle Analysis[1]

Cell Line: AsPC1 and MIA-PaCa-2 cells
Concentration: 4 and 6 μM
Incubation Time: 72 h
Result: The proportion of G1 phase cells increased by 20-30%.

RT-PCR[1]

Cell Line: AsPC1 and MIA-PaCa-2 cells
Concentration: 6 μM
Incubation Time: 48 h
Result: Increased the levels of CDKN1A, DDIT3, IL-1β, PMAIP1 and CASP4.

Western Blot Analysis[1]

Cell Line: AsPC1 and MIA-PaCa-2 cells
Concentration: 4 and 6 μM
Incubation Time: 72 h
Result: Decreased the levels of p-DDR2 and p-ERK.
Increased the level of cleaved caspase-3.
In Vivo

CIDD-8633 (40 mg/kg, i.p., twice a week for 28 days) exerts anti-tumor effects by targeting DDR2 in mouse models established from MIA PaCa-2 cells and Pan02 cells respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MIA PaCa-2 induced PDAC model established in NOD/SCID mice[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection (i.p.), twice a week for 28 days
Result: Significant decreased the tumor weight and volume.
Decreased the levels of p-DDR2 and p-ERK.
Animal Model: Pan02 induced PDAC model established in C57BL/6J mice[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection (i.p.), twice a week for 28 days
Result: Delayed the tumor growth.
Decreased the levels of p-DDR2 and p-ERK.
Molecular Weight

445.48

Formula

C22H23N9O2
CAS No.
SMILES

O=C(NC1=CC=C(NC2=NC(NCC)=NC(C)=C2)C=C1)COC(C=C3)=NN=C3N4C=CC=N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CIDD-8633 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CIDD-86331428356-95-9CIDD8633CIDD 8633Discoidin Domain ReceptorApoptosisCaspaseInterleukin RelatedILARDSanti-inflammationzebrafishischemia-reperfusion injurymiceInhibitorinhibitorinhibit

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