LBW242


Catalog No. Size PriceQuantity
M17588-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer drug-mediated cell death of ovarian cancer cells.

Product information

CAS Number: 867324-12-7

Molecular Weight: 454.65

Formula: C27H42N4O2

Chemical Name: (2S)-N-[(1S)-2-[(3aR,7aS)-6-(2-phenylethyl)-octahydro-1H-pyrrolo[2,3-c]pyridin-1-yl]-1-cyclohexyl-2-oxoethyl]-2-(methylamino)propanamide

Smiles: C[C@H](NC)C(=O)N[C@@H](C1CCCCC1)C(=O)N1CC[C@H]2CCN(C[C@@H]12)CCC1C=CC=CC=1

InChiKey: HCSMRSHIIKPNAK-LSAVBLLPSA-N

InChi: InChI=1S/C27H42N4O2/c1-20(28-2)26(32)29-25(23-11-7-4-8-12-23)27(33)31-18-15-22-14-17-30(19-24(22)31)16-13-21-9-5-3-6-10-21/h3,5-6,9-10,20,22-25,28H,4,7-8,11-19H2,1-2H3,(H,29,32)/t20-,22+,24+,25-/m0/s1

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

How to use

In Vitro:

LBW242 is a 3-mer and Smac mimetic, based on the ability of the NH2-terminal seven amino acids of Smac to neutralize the BIR3 domain of X-chromosome-linked IAP (XIAP). LBW242 partially inhibits the growth of mutant FLT3-expressing lines, MV4;11 at 1 μM. LBW242 kills cells in a manner strictly dependent on caspases, and death is accompanied by PARP cleavage, Annexin positivity, and accumulation of cells in sub-G1. LBW242 (0-0.1 μM; 3 days) inhibits a panel of PKC412-sensitive or PKC412-resistant, mutant FLT3-expressing Ba/F3 lines The IC50 values ranged from 0.5 to >1 μM.

In Vivo:

LBW242 (50 mg/kg; p.o.; daily for 10 days) reduces tumor burden.

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

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