LTX-315 (KKWWKKW-Dip-K-NH2) is an oncolytic peptide with potent anticancer activity; inhibits MRC-5, A20 and AT84 with IC50s of 34.3, 8.3 and 11 μM, respectively.

Product information

CAS Number: 1345407-05-7

Molecular Weight: 1439.79

Formula: C78H106N18O9

Chemical Name: (2S)-6-amino-2-[(2S)-2-[(2S)-2-[(2S)-6-amino-2-[(2S)-6-amino-2-[(2S)-2-[(2S)-2-[(2S)-6-amino-2-[(2S)-2,6-diaminohexanamido]hexanamido]-3-(1H-indol-3-yl)propanamido]-3-(1H-indol-3-yl)propanamido]hexanamido]hexanamido]-3-(1H-indol-3-yl)propanamido]-3,3-diphenylpropanamido]hexanamide

Smiles: NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC1=CNC2=CC=CC=C12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC1=CNC2=CC=CC=C12)NC(=O)[C@H](CC1=CNC2=CC=CC=C12)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CCCCN)C(C1C=CC=CC=1)C1C=CC=CC=1

InChiKey: GGAKLYWEFZCVIT-TVEKFXMRSA-N

InChi: InChI=1S/C78H106N18O9/c79-38-18-13-30-57(84)71(98)90-62(35-15-20-40-81)73(100)93-66(44-52-47-87-59-32-11-8-28-55(52)59)76(103)95-65(43-51-46-86-58-31-10-7-27-54(51)58)75(102)92-63(36-16-21-41-82)72(99)91-64(37-17-22-42-83)74(101)94-67(45-53-48-88-60-33-12-9-29-56(53)60)77(104)96-69(78(105)89-61(70(85)97)34-14-19-39-80)68(49-23-3-1-4-24-49)50-25-5-2-6-26-50/h1-12,23-29,31-33,46-48,57,61-69,86-88H,13-22,30,34-45,79-84H2,(H2,85,97)(H,89,105)(H,90,98)(H,91,99)(H,92,102)(H,93,100)(H,94,101)(H,95,103)(H,96,104)/t57-,61-,62-,63-,64-,65-,66-,67-,69-/m0/s1

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : ≥ 50 mg/mL (34.73 mM). H2O : 100 mg/mL (69.45 mM; Need ultrasonic).

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:

LTX-315 is found to be equipotent against drug-resistant cancer cells, nontoxic towards red blood cells, shows high plasma protein binding and is quite rapidly degraded to non-toxic metabolites. LTX-315 induces rapid killing of cancer cells. The oncolytic activity of LTX-315 stems from both a direct lytic effect on the plasma membrane in addition to permeabilization of the mitochondrial membrane, leading to cellular death by necrosis and release of tumor antigens. Treatment of cancer cells with LTX-315 causes the release of several danger signals (DAMPs) that are associated with immunogenic cell death and stimulation of adaptive immune responses.

In Vivo:

Intratumoral administration of LTX-315 has resulted in complete regression and systemic tumor specific immune responses in several preclinical models. Intratumoral administration of LTX-315 resulted in tumor necrosis and the infiltration of immune cells into the tumor parenchyma followed by complete regression of the tumor in the majority of the animals. LTX-315 induced the release of danger-associated molecular pattern molecules such as the high mobility group box-1 protein in vitro and the subsequent upregulation of proinflammatory cytokines such as interleukin (IL) 1β, IL6 and IL18 in vivo. Animals cured by LTX-315 treatment are protected against a re-challenge with live B16 tumor cells both intradermally and intravenously.

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