LB42708


Catalog No. Size PriceQuantity
M22499-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

LB42708 is a selective inhibitor of farnesyltransferase (FTase) with IC50 value of 0.8nM . LB42708 is a nonpeptide pyrrole-based FTase inhibitor with high potency and selectivity. It inhibits the farnesylation of H-ras, N-ras and K-ras4B in vitro with IC50 values of 0.8nM, 1.2nM and 2nM, respectively. To the related enzyme geranylgeranyltransferase I, LB42708 shows no significant inhibition with IC50 value of 100μM. In cultured RAW264.7 cell line, LB42708 potently reduces the farnesylated p21ras stimulated by LPS and IFN-γ with IC50 value of ~ 10nM. Besides that, the HUVEC cells treated with LB42708 shows inhibition of cell proliferation and migration induced by VEGF. LB42708 inhibits the VEGF-induced DNA synthesis with IC50 value of 75nM and also inhibits VEGF-induced formation of the GTP-bound form of Ras with IC50 values of 50nM. In addition, it affects the tube-like structure formation. Furthermore, the administration of LB42708 can suppress tumor growth both in Ras-mutated HCT116 and wild-type Caco-2 xenograft models [1, 2].

Product information

CAS Number: 226929-39-1

Molecular Weight: 555.46

Formula: C30H27BrN4O2

Chemical Name: 4-[1-({1-[(4-bromophenyl)methyl]-1H-imidazol-5-yl}methyl)-4-(naphthalen-1-yl)-1H-pyrrole-3-carbonyl]morpholine

Smiles: O=C(C1=CN(CC2=CN=CN2CC2C=CC(Br)=CC=2)C=C1C1=CC=CC2=CC=CC=C21)N1CCOCC1

InChiKey: GUUIRIMAQGOLHT-UHFFFAOYSA-N

InChi: InChI=1S/C30H27BrN4O2/c31-24-10-8-22(9-11-24)17-35-21-32-16-25(35)18-33-19-28(27-7-3-5-23-4-1-2-6-26(23)27)29(20-33)30(36)34-12-14-37-15-13-34/h1-11,16,19-21H,12-15,17-18H2

Technical Data

Appearance: Solid Power

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

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

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

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