SP 141 (Synonyms: AGN-PC-0D106I) |
| Catalog No.GC10022 |
Mdm2 inhibitor
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.
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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.
| Cas No. | 1253491-42-7 | SDF | |
| Synonyms | AGN-PC-0D106I | ||
| Chemical Name | 6-methoxy-1-(1-naphthalenyl)-9H-pyrido[3,4-b]indole | ||
| Canonical SMILES | COC1=CC2=C(C=C1)NC(C2=CC=N3)=C3C4=C(C=CC=C5)C5=CC=C4 | ||
| Formula | C22H16N2O | M.Wt | 324.4 |
| Solubility | ≤100mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0826 mL | 15.4131 mL | 30.8261 mL |
| 5 mM | 0.6165 mL | 3.0826 mL | 6.1652 mL |
| 10 mM | 0.3083 mL | 1.5413 mL | 3.0826 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)
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