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製品番号: 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 ligand (HY-189438); Blue: Cereblon ligand (HY-189439); Black: linker).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 3063346-83-5
分子式: C₄₃H₄₉F₂N₉O₄
分子量:793.90

保管条件:

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

Data Sheet (270 KB)

LRK-4189 構造式

CAS 番号: 3063346-83-5

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性

製品説明

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 ligand (HY-189438); Blue: Cereblon ligand (HY-189439); Black: linker).

PROTACs アイソフォーム固有の製品をすべて表示 :

体外実験

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.

体内実験

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.

臨床実験

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

化学情報

CAS 番号 3063346-83-5
分子量 793.90
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (270 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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希釈計算機

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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.

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MOQ

Minimum order quantity

100 mg

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