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Product introduction

Bemcentinib (R428, BGB324)是一种Axl抑制剂，IC50为14 nM，作用于Axl比作用于Abl选择性高100倍以上。作用于Axl选择性也比作用于Mer和Tyro3(高50到100倍)及InsR， EGFR， HER2，和PDGFRβ(高100倍以上)高。 R428是一种选择性的Axl抑制剂，IC50值为14 nM。与Abl、Mer、Tyro3、InsR、EGFR、HER2和PDGFR相比，R428对Axl具有超过50倍的灵敏度。 Axl受体酪氨酸激酶通过结合维生素K依赖性蛋白growth arrest-specific 6 (Gas6)将细胞外基质信号传导到胞浆内。Axl参与多个细胞内进程，包括细胞生长、迁移、聚集和抗炎活性。 R428在低纳摩尔浓度下就可以阻断Axl的催化活性，同时抑制Axl依赖的活性，包括Akt磷酸化、细胞侵袭、促炎因子的产生。R428可以减少粒细胞巨噬细胞集落刺激因子和上皮-间质转化转录因子Snail的表达。R428还可以抑制血管生成，减少转移性肿瘤负荷，在动物异种移植模型中提高生存率。此外，R428与cisplatin协同作用可以提高肝脏微转移的抑制效率。

Specs ⸢ View details ⸥

Chinese name

贝森替尼, 酪氨酸蛋白激酶受体 UFO 抑制剂

English name

R428 (BGB324)

Chinese alias

奎利珠单抗

English alias

BGB324; BGB-324; BGB 324; R 428; R-428; Bemcentinib | NSC824183 | NSC-824183 | BCP21180 | R428 | R-428 | GTPL10478 | W-105659 | 1H-1,2,4-Triazole-3,5-diamine, 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-py

CAS number

1037624-75-1

molecular formula

C30H34N8

molecular weight

506.64 g/mol

Exact mass

PSA

97.800 Å²

Logp

5.5

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R428 (BGB324) 10mM in DMSO 1ml

Name: R428 (BGB324) 10mM in DMSO 1ml
Brand: 麦克林
SKU: R798238-1ml

R428 (BGB324) 10mM in DMSO 1ml Macklin 1037624-75-1, complete specifications, for production, research, laboratory testing and inspection, digital one-stop procurement platform for scientific materials.

item number：R798238-1ml

Product model：1ml

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Lead Time：30days

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R428 (BGB324) 10mM in DMSO 1ml

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