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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-GPC-100 hydrobromide
GPC-100 hydrobromide

Chemical Structure : GPC-100 hydrobromide

CAS No.: 1191450-19-7

GPC-100 hydrobromide (TG-0054, Burixafor)

货号: PC-21292Not For Human Use, Lab Use Only.

GPC-100 (TG-0054, Burixafor) is a novel small molecule antagonist of CXCR4, shows competitive inhibition of CXCL12 binding to CXCR4 with Ki of 1.6 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GPC-100 (TG-0054, Burixafor) is a novel small molecule antagonist of CXCR4, shows competitive inhibition of CXCL12 binding to CXCR4 with Ki of 1.6 nM.
GPC-100 (TG-0054, Burixafor) demonstrates distinct divergence from AMD3100, and has a higher affinity for CXCR4 than AMD3100 (Ki=40 nM).
GPC-100 (TG-0054, Burixafor) dose dependenlyt inhibits CXCL12-induced calcium flux in MDA-MB-231 cells overexpressing CXCR4 with IC50 value of 30 nM.
GPC-100 (TG-0054, Burixafor) inhibits CXCL12 mediated recruitment of β-arrestin to CXCR4 with IC50 value of 207 nM in the PRESTO-TANGO β-arrestin assay.
GPC-100 (TG-0054, Burixafor) efficiently blocks CXCL12-mediated migration in U937 and MM.1S cells with IC50 of 48 nM and 28 nM, respectively.

物理化学性质&存储条件

分子量 647.64
分子式 C27H52BrN8O3P
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Phosphonic acid, P-[2-[4-[6-amino-2-[[[trans-4-[[[3-(cyclohexylamino)propyl]amino]methyl]cyclohexyl]methyl]amino]-4-pyrimidinyl]-1-piperazinyl]ethyl]-, hydrobromide

参考文献

1. Sukhtankar DD, et al. PLoS One. 2023 Oct 25;18(10):e0287863.

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