LB42908 | CAS#226927-89-5 | Farnesyltransferase inhibitor

MedKoo Cat#: 406419 | Name: LB42908

Description:

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

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

LB42908

CAS#226927-89-5

Theoretical Analysis

MedKoo Cat#: 406419

Name: LB42908

CAS#: 226927-89-5

Chemical Formula: C32H31N5O3

Exact Mass: 533.2427

Molecular Weight: 533.62

Elemental Analysis: C, 72.03; H, 5.86; N, 13.12; O, 8.99

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

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

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 533.62 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.

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

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.