SP 141

SP-141 is a MDM2 inhibitor. It acts by exerting excellent in-vitro and in-vivo anticancer activity.

Product information

CAS Number: 1253491-42-7

Molecular Weight: 324.38

Formula: C22H16N2O

Chemical Name: 6-Methoxy-1-naphthalen-1-yl-9H-pyrido[3, 4-b]indole

Smiles: COC1C=C2C(=CC=1)NC1=C(N=CC=C21)C1=CC=CC2=CC=CC=C21

InChiKey: AABFWJDLCCDJJN-UHFFFAOYSA-N

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

SP141, which bound directly to MDM2, promoting its auto-ubiquitination and degradation by the proteasome. The compound reduced levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation, with 50% inhibitory concentrations <0.5 μM (0.38-0.50 μM). Increasing concentrations of SP141 induced increasing levels of apoptosis and G2-M-phase arrest of pancreatic cancer cell lines, whether or not they expressed functional P53.

In Vivo:

Injection of nude mice with SP141 (40 mg/kg/d) inhibited growth of xenograft tumors (by 75% compared with control mice), and led to regression of orthotopic tumors.

References:

1. Wei Wang, 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.
2. Wei Wang , 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.

Products are for research use only. Not for human use.