2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. Bemcentinib (GMP)

Bemcentinib (GMP)  (Synonyms: R428 (GMP); BGB324 (GMP))

目录号: HY-15150G
产品使用指南 技术支持

Bemcentinib (R428) GMP 是 GMP 级别的 Bemcentinib (HY-15150)。GMP 级别的小分子可用做细胞疗法中的辅助试剂。Bemcentinib (R428) 是一种选择性具有口服活性的 Axl 抑制剂，IC50 为 14 nM。Bemcentinib 可抑制癌细胞迁移和侵袭。在细胞中，Bemcentinib 对 Axl 的选择性是 Abl 的 100 倍以上，对 TAM 家族激酶 Mer 和 Tyro3 的选择性分别为 50 倍和 100 倍以上。Bemcentinib 可阻断转移性乳腺癌模型中的肿瘤扩散并延长生存期。

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Bemcentinib (GMP)

Bemcentinib (GMP) Chemical Structure

CAS No. : 1037624-75-1

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Bemcentinib (GMP) 相关抗体

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查看 TAM Receptor 亚型特异性产品:

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Axl Mer Tyro3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bemcentinib (R428) GMP is Bemcentinib (HY-15150) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy.Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer[1][2].

IC50 & Target

Axl

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
4T1 IC50
0.94 μM
Compound: 1; R428, BGB-324
Antiproliferative activity against mouse 4T1 cells highly expressing AXL after 72 hrs by MTT assay
Antiproliferative activity against mouse 4T1 cells highly expressing AXL after 72 hrs by MTT assay
[PMID: 35279611]
BaF3 IC50
117.2 nM
Compound: 2; BGB324
Antiproliferative activity against mouse BaF3/TEL-AXL cells incubated for 72 hrs by SRB or CCK8 assay
Antiproliferative activity against mouse BaF3/TEL-AXL cells incubated for 72 hrs by SRB or CCK8 assay
[PMID: 33733758]
BaF3 IC50
117.2 nM
Compound: 8; R428; BGB324
Antiproliferative activity against mouse BaF3 stably expressing human TEL-AXL incubated for 72 hrs
Antiproliferative activity against mouse BaF3 stably expressing human TEL-AXL incubated for 72 hrs
[PMID: 33957388]
BaF3 IC50
98.8 nM
Compound: 1; BGB324
Antiproliferative activity against mouse BaF3 cells transfected with TEL-AXL assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells transfected with TEL-AXL assessed as inhibition of cell growth incubated for 72 hrs
[PMID: 36358010]
GES1 IC50
> 60 μM
Compound: 1; R428, BGB-324
Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
[PMID: 35279611]
HeLa IC50
< 30 nM
Compound: 17; BGB324; R428
Inhibition of recombinant AXL in human HeLa cells after 1 hr by ELISA
Inhibition of recombinant AXL in human HeLa cells after 1 hr by ELISA
[PMID: 26555154]
MCF-10A IC50
> 60 μM
Compound: 1; R428, BGB-324
Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
[PMID: 35279611]
MDA-MB-231 IC50
2.84 μM
Compound: 1; R428, BGB-324
Antiproliferative activity against human MDA-MB-231 cells highly expressing AXL after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells highly expressing AXL after 72 hrs by MTT assay
[PMID: 35279611]
体外研究
(In Vitro)

Bemcentinib (R428) (2 μM) 显著干扰 Axlpos 黑色素瘤细胞的迁移和侵袭机制，其水平与 Axl 敲低相当[1]。
Bmcentinib (R428) 协同 CDDP 增强肝脏微转移抑制作用[2]。
Bmcentinib (R428) (50 nM-1 μM) 可引起前脂肪细胞向成熟脂肪细胞分化的浓度依赖性抑制，这可以通过降低脂质摄取得到证明[3]。

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

Bemcentinib (GMP) 相关抗体:
体内研究
(In Vivo)

Bemcentinib (R428) (125 mg/kg, p.o.) 显著阻断 MDA-MB-231-luc-D3H2LN 在两种独立小鼠乳腺癌扩散模型中的转移发展，抑制肿瘤血管生成和血管内皮生长因子 (VEGF) 诱导的角膜新生血管生成[2]。
Bemcentinib (R428) (75 mg/kg/day, 25 mg/kg twice daily, p.o.) 让老鼠保持高脂肪饮食导致体重增加和皮下和性腺脂肪量显著减少[3]。

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

506.64

Formula

C30H34N8
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

Bemcentinib (GMP) 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:

Bemcentinib (GMP)1037624-75-1R428 (GMP)BGB324 (GMP)TAM ReceptorTyro3AxlMerbreast cancerlung cancerMDA-MB-231CDDPmelanomaInhibitorinhibitorinhibit

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