LB42908

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406419

CAS#: 226927-89-5

Description: LB42908 is a highly potent Ras farnesyltransferase inhibitor(IC(50)=0.9 nM against H-Ras and 2.4 nM against K-Ras) with potential anticancer activity.


Chemical Structure

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LB42908
CAS# 226927-89-5

Theoretical Analysis

MedKoo Cat#: 406419
Name: LB42908
CAS#: 226927-89-5
Chemical Formula: C32H31N5O3
Exact Mass: 533.24269
Molecular Weight: 533.62024
Elemental Analysis: C, 72.03; H, 5.86; N, 13.12; O, 8.99

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Synonym: LB42908; LB-42908; LB 42908.

IUPAC/Chemical Name: (1-((1-(benzo[d][1,3]dioxol-5-ylmethyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(4-methylpiperazin-1-yl)methanone

InChi Key: HWLBLFBLGGVDBT-UHFFFAOYSA-N

InChi Code: InChI=1S/C32H31N5O3/c1-34-11-13-36(14-12-34)32(38)29-20-35(19-28(29)27-8-4-6-24-5-2-3-7-26(24)27)18-25-16-33-21-37(25)17-23-9-10-30-31(15-23)40-22-39-30/h2-10,15-16,19-21H,11-14,17-18,22H2,1H3

SMILES Code: O=C(C1=CN(CC2=CN=CN2CC3=CC=C(OCO4)C4=C3)C=C1C5=C6C=CC=CC6=CC=C5)N7CCN(C)CC7

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 533.62024 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Moorthy NS, Sousa SF, Ramos MJ, Fernandes PA. Farnesyltransferase inhibitors: a comprehensive review based on quantitative structural analysis. Curr Med Chem. 2013;20(38):4888-923. PubMed PMID: 24059235.

2: Chang M, Lee SH, Kim HJ, Koh JS, Kim A. Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities. Bioorg Med Chem Lett. 2012 May 1;22(9):3067-71. doi: 10.1016/j.bmcl.2012.03.070. Epub 2012 Mar 27. PubMed PMID: 22497764.

3: Lee SK, Han YM, Yun J, Lee CW, Shin DS, Ha YR, Kim J, Koh JS, Hong SH, Han DC, Kwon BM. Phosphatase of regenerating liver-3 promotes migration and invasion by upregulating matrix metalloproteinases-7 in human colorectal cancer cells. Int J Cancer. 2012 Aug 1;131(3):E190-203. doi: 10.1002/ijc.27381. Epub 2012 Jan 11. PubMed PMID: 22131018.

4: Kim HS, Kim JW, Gang J, Wen J, Koh SS, Koh JS, Chung HH, Song SY. The farnesyltransferase inhibitor, LB42708, inhibits growth and induces apoptosis irreversibly in H-ras and K-ras-transformed rat intestinal epithelial cells. Toxicol Appl Pharmacol. 2006 Sep 15;215(3):317-29. Epub 2006 May 19. PubMed PMID: 16712893.

5: Lee SK, Kim JM, Lee MY, Son KH, Yeom YI, Kim CH, Shin Y, Koh JS, Han DC, Kwon BM. Confirmation of a linkage between H-Ras and MMP-13 expression as well as MMP-9 by chemical genomic approach. Int J Cancer. 2006 May 1;118(9):2172-81. PubMed PMID: 16331612.

6: Jin HT, Youn JI, Kim HJ, Lee JB, Ha SJ, Koh JS, Sung YC. Enhancement of interleukin-12 gene-based tumor immunotherapy by the reduced secretion of p40 subunit and the combination with farnesyltransferase inhibitor. Hum Gene Ther. 2005 Mar;16(3):328-38. PubMed PMID: 15812228.

7: Lee H, Lee J, Lee S, Shin Y, Jung W, Kim JH, Park K, Kim K, Cho HS, Ro S, Lee S, Jeong SW, Choi T, Chung HH, Koh JS. A novel class of highly potent, selective, and non-peptidic inhibitor of Ras farnesyltransferase (FTase). Bioorg Med Chem Lett. 2001 Dec 3;11(23):3069-72. PubMed PMID: 11714612.

LB42908

10.0mg / Not available


Additional Information