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Art. -Nr.: HY-175751

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LRK-4189

LRK-4189 is an first-in-class, orally active CRBN-dependent PIP4K2C PROTAC degrader. LRK-4189-mediated degradation of PIP4K2C leads to intrinsic cell death and upregulation of the STAT1 pathway and signaling in microsatellite stable colorectal cancer (MSS CRC) cells. LRK-4189 can be used for the research of microsatellite-stable colorectal cancer.
(Pink: PIP4K2C Target protein ligand; Blue: Cereblon E3 ligase ligand; Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3063346-83-5
Formel: C₄₃H₄₉F₂N₉O₄
Molecular Weight:793.90

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

LRK-4189 Chemical Structure

CAS. Nr.: 3063346-83-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

LRK-4189 is an first-in-class, orally active CRBN-dependent PIP4K2C PROTAC degrader. LRK-4189-mediated degradation of PIP4K2C leads to intrinsic cell death and upregulation of the STAT1 pathway and signaling in microsatellite stable colorectal cancer (MSS CRC) cells. LRK-4189 can be used for the research of microsatellite-stable colorectal cancer^[1]^[2]. (Pink: PIP4K2C Target protein ligand; Blue: Cereblon E3 ligase ligand; Black: linker).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

LRK-4189 (Compound 603) exhibits a 24 h DC₅₀ of <500 nM against PIP4K2C in MOLT-4 cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LRK-4189 reduces tumor growth and improves survival in multiple CRC mouse models and in ex vivo primary human CRC spheroids^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 3063346-83-5
Molecular Weight 793.90
Formel C₄₃H₄₉F₂N₉O₄
SMILES

O=C1CC[C@@H](C(N1)=O)NC2=CC=C(C(F)=C2)N3CCN(CC3)[C@H]4CC[C@@H](CC4)C(N[C@H]5CC[C@@H](CC5)NC6=NC(C7=CC=CC(N8C=CC=CC8=O)=C7)=C(C=N6)F)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Krista B. Goodman, et al. Abstract B042: Clinical development and mechanism of action of LRK-4189, a first-in-class degrader of the lipid kinase PIP4K2C. Clin Cancer Res (2026) 32 (14_Supplement): B042.

[2]. Krista Goodman, et al. Abstract CT052: Proof of mechanism from a phase 1, single ascending dose (SAD) study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of LRK-4189 in healthy subjects. Cancer Res (2026) 86 (8_Supplement): CT052.

[3]. Preparation of trisubstituted pyrimidine compounds as inhibitors and degraders of PIP4K protein. World Intellectual Property Organization, WO2024233846 A1.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise

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LRK-4189

Alle PROTACs Isoform-spezifische Produkte anzeigen