SP 141 (Synonyms: AGN-PC-0D106I) |
Catalog No.GC10022 |
SP 141 est un inhibiteur spécifique de MDM2. Le SP 141 favorise l'auto-ubiquitination et la dégradation de MDM2. Le SP 141 pourrait être utilisé pour la recherche sur le cancer du pancréas et les cellules cancéreuses du sein.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1253491-42-7
Sample solution is provided at 25 µL, 10mM.
SP 141 is a specific, potent and selective small-molecule antagonist of MDM2 with Ki value of 28±6 nM [2][3][4].
Mouse double minute 2 protein (Mdm2) is an ubiquitin ligase that promotes p53 degradation, a tumor suppressor that controls a major pathway protecting cells from malignant transformation [1].
SP 141 is a potent and selective MDM2 inhibitor. In breast cancer cell lines, SP-141 reduced cell viability with IC50 less than 1 μM (0.39-0.91 μM) and inhibited cancer cell colony formation in a concentration-dependent way. SP-141 also increased apoptosis and concentration-dependently inhibited cell proliferation. In both MCF-7 and MDA-MB-468 cells, SP-141 increased the degradation rate of the MDM2 protein [2].
In nude mice bearing MCF-7 and MDA-MB-468 xenograft tumours, intraperitoneal (i.p.) injection of SP-141 inhibited tumour growth by ~82% and ~80%, respectively [2]. In pancreatic xenograft and orthotopic mouse models, intraperitoneal (i.p.) injections of SP141 significantly inhibited the growth of pancreatic xenograft tumors and caused complete tumor regression of orthotopic pancreatic tumors [3]. In tumor-bearing nude mice, SP-141 had a short half-life in plasma and wide tissue distribution [4].
References:
[1]. Vassilev LT, Vu BT, Graves B, et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science. 2004 Feb 6;303(5659):844-8.
[2]. Wang W, Qin JJ, Voruganti S, et al. The pyrido[b]indole MDM2 inhibitor SP-141 exerts potent therapeutic effects in breast cancer models. Nat Commun. 2014 Oct 1;5:5086.
[3]. Wang W, Qin JJ, Voruganti S, et al. Identification of a new class of MDM2 inhibitor that inhibits growth of orthotopic pancreatic tumors in mice. Gastroenterology. 2014 Oct;147(4):893-902.e2.
[4]. Nag S, Qin JJ, Voruganti S, et al. Development and validation of a rapid HPLC method for quantitation of SP-141, a novel pyrido[b]indole anticancer agent, and an initial pharmacokinetic study in mice. Biomed Chromatogr. 2015 May;29(5):654-63.
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