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SP 141

 
Catalog No.
C4120
Mdm2抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,090.00
Ship with 10-15 days
10mg
¥ 1,745.00
Ship with 10-15 days
50mg
¥ 6,436.00
Ship with 10-15 days

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A

背景

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.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt324.4
Cas No.1253491-42-7
FormulaC22H16N2O
SynonymsAGN-PC-0D106I
Solubility≤100mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide
Chemical Name6-methoxy-1-(1-naphthalenyl)-9H-pyrido[3,4-b]indole
SDFDownload SDF
Canonical SMILESCOC1=CC2=C(C=C1)NC(C2=CC=N3)=C3C4=C(C=CC=C5)C5=CC=C4
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质量控制

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化学结构

SP 141