SP 141
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 324.4 |
Cas No. | 1253491-42-7 |
Formula | C22H16N2O |
Synonyms | AGN-PC-0D106I |
Solubility | ≤100mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide |
Chemical Name | 6-methoxy-1-(1-naphthalenyl)-9H-pyrido[3,4-b]indole |
SDF | Download SDF |
Canonical SMILES | COC1=CC2=C(C=C1)NC(C2=CC=N3)=C3C4=C(C=CC=C5)C5=CC=C4 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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