| Identification | Back Directory | [Name]
SP 141 | [CAS]
1253491-42-7 | [Synonyms]
SP 141
SP 141;SP141;
6-Methoxy-1-(1-naphthyl)-9H-β-carboline
6-Methoxy-1-(1-naphthalenyl)-9H-pyrido[3,4-b]indole
9H-Pyrido[3,4-b]indole, 6-methoxy-1-(1-naphthalenyl)- | [Molecular Formula]
C22H16N2O | [MDL Number]
MFCD29059920 | [MOL File]
1253491-42-7.mol | [Molecular Weight]
324.38 |
| Chemical Properties | Back Directory | [Boiling point ]
571.2±45.0 °C(Predicted) | [density ]
1.284±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≤100mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide | [form ]
crystalline solid | [pka]
15.04±0.40(Predicted) | [color ]
White to yellow | [InChI]
1S/C22H16N2O/c1-25-15-9-10-20-19(13-15)18-11-12-23-21(22(18)24-20)17-8-4-6-14-5-2-3-7-16(14)17/h2-13,24H,1H3 | [InChIKey]
AABFWJDLCCDJJN-UHFFFAOYSA-N | [SMILES]
COC1=CC=C(NC2=C3C=CN=C2C4=CC=CC5=C4C=CC=C5)C3=C1 |
| Hazard Information | Back Directory | [Description]
Mouse double minute 2 protein (MDM2) is an E3 ubiquitin-protein ligase that binds and ubiquitinates the tumor suppressor p53, leading to its degradation by the proteasome. SP 141 is a cell-permeable inhibitor of MDM2 (Ki = 28 nM). Binding of MDM2 by SP 141 promotes its auto-ubiquitination and proteasomal degradation. SP 141 induces cell cycle arrest and apoptosis in breast and pancreatic cancer cell lines and inhibits xenograft tumor growth in vivo. This compound has a short half-life in plasma and wide tissue distribution in tumor-bearing nude mice. | [Uses]
SP 141 induces cell cycle arrest and apoptosis in breast and pancreatic cancer cell lines, inhibiting xenograft tumor growth in vivo. | [in vivo]
SP-141 (40 mg/kg; administered by i.p. injection; 5 d/wk for about three weeks) suppresses pancreatic tumor growth in both xenograft and orthotopic mouse models[1].
| Animal Model: | Nude mice bearing Panc-1 xenograft tumors[1] | | Dosage: | 40 mg/kg | | Administration: | Administered by i.p. injection; 5 d/wk for about three weeks | | Result: | Significantly suppressed the growth of pancreatic xenograft tumors. On Day 18, the tumor volume in the treated group was reduced by 75% compared with that in the control group. There were no significant differences in the body weight compared with the control group. |
| [storage]
Store at -20°C | [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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| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|