"目录号: HY-13696
GPCR/G ProteinImmunology/Inflammation-
MSX-122是一种新型小分子CXCR4 拮抗剂, 有效抑制 CXCR4/CXCL12 (IC50值为10 nM)。
CXCR
相关产品
Plerixafor octahydrochloride-Reparixin-SCH 527123-Danirixin-SCH 546738-AMD 3465 hexahydrobromide-AMG 487-SB225002-AMD-070 hydrochloride-SCH 563705-NBI-74330-LY2510924-WZ811-IT1t dihydrochloride-SRT3109-
生物活性
Description
MSX-122 is a novel small molecule and partial CXCR4 antagonist, with potent inhibition of CXCR4/CXCL12 actions (IC50 = 10 nM).IC50 value: 10 nM Target: CXCR4/CXCL12in vitro: MSX-122 is a partial inhibitor of CXCR4/CXCL12 functions. The compelling features of the MSX-122 profile include: (i) potent inhibition of CXCR4/CXCL12 actions (IC50 = 10 nM); (ii) ease of production on a large scale; (iii) effectiveness as an anti-inflammatory and anti-metastatic agent in vivo; and (iv) unique property of blocking homing and recruitment without mobilizing stem cells. MSX-122 blocks invasion and angiogenesis in vitro.in vivo: MSX-122 attenuates colonic damage in mice with experimental colitis.MSX-122 blocks metastasis in an experimental animal model of breast cancer metastasis. MSX-122 blocks metastasis in two more animal models for metastasis.
Clinical Trial
NCT00591682
Metastatix, Inc.
Solid Tumors
November 2007
Phase 1
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References
[1].Liang Z, et al. Development of a unique small molecule modulator of CXCR4. PLoS One. 2012;7(4):e34038.