2. GPCR/G Protein Immunology/Inflammation MAPK/ERK Pathway Stem Cell/Wnt PI3K/Akt/mTOR
  3. CXCR ERK Akt
  4. BPRCX807

BPRCX 807 是一种选择性强效的 CXCR4 (CXC 趋化因子受体 4 型) 拮抗剂。BPRCX 807 可抑制 CXCL12 介导的 ERK 和 Akt 磷酸化。BPRCX 807 能显著抑制原发肿瘤的生长。BPRCX 807 可用于肝细胞癌的研究。

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BPRCX807

BPRCX807 Chemical Structure

CAS No. : 2236595-58-5

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BPRCX807 相关抗体

Top Publications Citing Use of Products

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

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ERK ERK1 ERK2 ERK5 ERK8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BPRCX 807 is a selective and potent CXCR4 (CXC chemokine receptor type 4) antagonist. BPRCX 807 inhibits CXCL12-mediated ERK and Akt phosphorylation. BPRCX 807 can significantly suppress primary tumor growth. BPRCX 807 can be used for the study of hepatocellular carcinoma[1].

IC50 & Target[1]

CXCR4

 

体外研究
(In Vitro)

BPRCX 807 (1.5 小时) 对 HEK293T 细胞的 IC50 值为 40.4 nM[1]。
BPRCX 807 对 CCRF-CEM 细胞的 EC50 值为 48.1 nM[1]。
BPRCX 807 (10 μM，24-72 小时) 显著抑制 CXCL12 诱导的 HCA-1 细胞伤口愈合加速[1]。
BPRCX 807 (0.1-1 μM，17.5 小时) 在 1 μM 浓度下显著减少 HCA-1 细胞的迁移数量[1]。
BPRCX 807 (10-20 μM，24-48 小时) 以剂量依赖的方式抑制缺氧诱导的 HCA-1 细胞间质标志物表达增加，并减轻缺氧诱导的 HCA-1 细胞上皮标志物表达降低[1]。
BPRCX 807 (5-20 μM, 24 h) 显著抑制 HCA-1 和 JHH-7 细胞中 CXCL12 介导的 ERK 和 Akt 磷酸化[1]。

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

BPRCX807 相关抗体:

Cell Migration Assay [1]

Cell Line: HCA-1 cells
Concentration: 10 μM
Incubation Time: 0 h, 24 h, 48 h, 72 h
Result: Significantly inhibited CXCL12-induced accelerated wound closure in HCA-1 cells.

Real Time qPCR[1]

Cell Line: Hypoxia-induced HCA-1 cells
Concentration: 10 μM, 20 μM
Incubation Time: 24 h, 48 h
Result: Increased in mesenchymal marker expression (including Slug, Fibronectin, N-cadherin, Vimentin, FOXC2, Zeb1, and Zeb2).
Alleviated the hypoxia-induced decrease in epithelial markers (E-cadherin, MTA-3, CLDN3, and CLDN5).
体内研究
(In Vivo)

BPRCX 807 (15 mg/kg，皮下注射，每日一次，连续 14 天) 单独使用或与 Sorafenib (HY-10201) 联合使用，可显著抑制 HCA-1 细胞同种异体移植和 JHH-7 细胞异种移植小鼠模型中的肿瘤生长[1]。
BPRCX 807 (15 mg/kg，皮下注射，每日一次，连续 14 天) 与抗 PD-1 抗体联合使用时，可募集 T 细胞，并协同抑制 HCA-1 细胞同种异体移植小鼠的肿瘤生长[1]。

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

Animal Model: HCA-1 or JHH-7 cells were orally implanted into the livers of 7-week-old C3H/HeNCrNarl mice and 9-week-old BALB/cAnN.Cg Foxnlnu/CrlNarl mice, respectively[1].
Dosage: 15 mg/kg
Administration: S.c., once daily for 14 days
Result: Significantly inhibited tumor growth when used alone.
The effect is strongest when used in combination with sorafenib.
Combined use significantly prolongs overall survival.
Reduced tumor-associated macrophage (TAM) infiltration (F4/80+ cells).
Reprogramed TAMs to the M1 phenotype (increased CD86+) and suppresses the M2 phenotype (decreased CD206+).
Increased cytotoxic CD8+ T cell infiltration.
Animal Model: HCA-1 cells were in situ implanted into 7-week-old C3H/HeNCrNarl mice. For combined anti-PD-1 immunotherapy, mice were intraperitoneally injected with anti-mouse PD-1 antibodies 10 days after tumor implantation[1].
Dosage: 15 mg/kg
Administration: S.c., once daily for 14 days
Result: When used in combination with Anti-PD-1, it significantly increased the infiltration of CD4+ and CD8+ T cells within tumors.
Synergistically inhibited tumor growth (reducing it by 95%) and lung metastasis.
分子量

613.79

Formula

C31H51N9O4
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

BPRCX807 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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:

BPRCX8072236595-58-5BPRCX 807BPRCX-807CXCRERKAktCXC chemokine receptorsC-X-C motif chemokine receptorsExtracellular signal regulated kinasesPKBProtein kinase Bhepatocellular carcinomaCXCR4 receptorprogrammed cell death 1sorafenibtumor microenvironmentInhibitorinhibitorinhibit

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