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製品番号: HY-189441

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ISM-PR25

ISM-PR25 is an orally active PROTAC degrader targeting BTK, with a DC₅₀ of 0.04 nM in Ramos cells. ISM-PR25 degrades BTK protein via CRL4^CRBN E3 ligase-mediated ubiquitination. ISM-PR25 can be used for research on B-cell lymphoma.
(Pink: Btk ligand (HY-170324); Blue: Cereblon E3 ligase ligand; 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。

分子式: C₅₀H₅₉N₁₁O₆
分子量:910.07

保管条件:

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

ISM-PR25 構造式

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
- IC₅₀ & Target
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

ISM-PR25 is an orally active PROTAC degrader targeting BTK, with a DC₅₀ of 0.04 nM in Ramos cells. ISM-PR25 degrades BTK protein via CRL4^CRBN E3 ligase-mediated ubiquitination. ISM-PR25 can be used for research on B-cell lymphoma^[1]. (Pink: Btk ligand (HY-170324); Blue: Cereblon E3 ligase ligand; Black: linker).

IC₅₀ & Target

^[1]

BTK

0.04 nM (DC₅₀)

PROTACs アイソフォーム固有の製品をすべて表示 :

体外実験

Anti-cancerOthers

Anti-cancer

ISM-PR25 (compound 25) (4 h) degrades BTK in Ramos cells with a DC₅₀ of 0.04 nM^[1].
ISM-PR25 (120 h) inhibits the viability of TMD8 cells expressing wild-type and mutant BTK, with IC₅₀ values of 5.6, 2.5, 9.0, and 10 nM, respectively^[1].

Others

ISM-PR25 binds to CRBN with an IC₅₀ of 93 nM^[1].
ISM-PR25 (7 days) shows a CTG HSC IC₅₀ of 398 nM in human CD34⁺ hematopoietic stem cells^[1].
ISM-PR25 (0.41 nM; 15 min) induces BTK/CRBN/PROTAC ternary complex formation with an EC₅₀ of 0.41 nM^[1].

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

Parmacokinetics

Species	Dose	Route	AUC_0-t	C_max	T_1/2	F
Mice^[1]	1 mg/kg	i.v.	18119 ng·h/mL	3903 ng/mL	2.0 h	26 %

体内実験

ISM-PR25 (compound 25) (3 mg/kg; p.o.; single administration) effectively degrades BTK in mouse circulating B cells^[1].

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

Animal Model:

BALB/c nude mice (female, 6-8 weeks)^[1]
Dosage:

3 mg/kg
Administration:

p.o.; single dose
Result:

Demonstrated a significant reduction of the BTK concentration in B-cells.
Showed comparable BTK degradation at both 2 h and 24 h, with efficacy at 24 h comparable to the reference NX-5948.

化学情報

分子量 910.07
分子式 C₅₀H₅₉N₁₁O₆
SMILES

O=C(C1=NC=C(N2C[C@H](N3CCN(C)C3=O)CCC2)N=C1NC4=CC=C(C5CCN(CC6=CC=C(CN([C@@]7(C)C(N([C@@H](CC8)C(NC8=O)=O)CC7)=O)C(C9=CC=CC=C9)=O)C=C6)CC5)C=C4)N
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

取扱説明書 (2659 KB)

参考文献

[1]. Mantsyzov AB, et al. Discovery of Highly Potent and Selective, Orally Bioavailable BTK-Targeting PROTACs Featuring Novel CRBN-Binding Warheads. Journal of medicinal chemistry. 2026 Sep 10;69(17):20494-20519. [Content Brief]

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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

Minimum order quantity

100 mg

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