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

CIDD-8633 是一种强效的 DDR2 抑制剂，其 IC50 值为 6.105 μM。CIDD-8633 显著抑制 MIA-PaCa-2 细胞和 AsPC-1 细胞的增殖，其 IC25 值分别为 4.0 和 5.5 μM。CIDD-8633 可抑制细胞迁移，阻滞细胞周期，诱导细胞凋亡 (apoptosis)，并显著抑制胰腺导管腺癌 (PDAC) 肿瘤的生长。CIDD-8633 可用于胰腺癌的研究，如 PDAC。

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CIDD-8633

CIDD-8633 Chemical Structure

CAS No. : 1428356-95-9

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CIDD-8633 相关抗体

Top Publications Citing Use of Products

查看 Discoidin Domain Receptor 亚型特异性产品:

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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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

CIDD-8633 (40°C-64°C) 可提高 AsPC-1、MIA、PaCa-2 和 KPC 细胞中 DDR2 蛋白的稳定性[1]。
CIDD-8633 (4-5.5 μM, 7-10 days) 可抑制 AsPC1 和 MIA-PaCa-2 细胞的长期克隆形成能力[1]。
CIDD-8633 (4-6 μM, 72 h) 可显著降低 AsPC1 和 MIA-PaCa-2 细胞中磷酸化 DDR2 及其下游效应分子磷酸化 ERK 的水平[1]。
CIDD-8633 (1.5 μM, 48 h) 可抑制 DDR2-ERK 信号通路的核转位，并阻断 AsPC1 和 MIA-PaCa-2 细胞中的增殖信号[1]。
CIDD-8633 (0.1-10 μM, 72 h) 可以剂量依赖性方式减少胰腺导管腺癌 (PDAC) 细胞的增殖[1]。
CIDD-8633 (4 μM, 16 h) 通过抑制 DDR2 降低 MIA PaCa-2 细胞的迁移能力[1]。
CIDD-8633 (4-6 μM, 72 h) 通过阻断 G1/S 期来抑制 AsPC1 和 MIA-PaCa-2 细胞的细胞周期进程[1]。
CIDD-8633 (4-6 μM, 72 h) 通过激活 caspase-3 诱导 AsPC1 和 MIA-PaCa-2 细胞凋亡[1]。
CIDD-8633 (6 μM, 48 h) 可上调 AsPC1 和 MIA-PaCa-2 细胞中包括 CDKN1A、DDIT3、IL-1β、PMAIP1 和CASP4 在内的基因[1]。
CIDD-8633 (4-10 μM, 72 h) 可显著降低 AsPC1 和 MIA-PaCa-2 细胞中 p-DDR2 和 p-ERK 的水平[1]。

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

CIDD-8633 相关抗体:

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.
体内研究
(In Vivo)

CIDD-8633 (40 mg/kg, i.p., 1 周 2 次, 共 28 天) 通过靶向 DDR2 分别在 MIA PaCa-2 细胞和 Pan02 细胞诱导的小鼠模型中发挥了抗肿瘤作用[1]。

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.
分子量

445.48

Formula

C22H23N9O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CIDD-8633 相关分类

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  • Do most proteins show cross-species activity?

    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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