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首頁 / / / / KT-474

KT-474 {[allProObj[0].p_purity_real_show]}

貨號：A1671259 同義名： PROTAC IRAK4 degrader-7; KYM-001

KT-474是一種 PROTAC IRAK4 降解劑，顯示出顯著的抗腫瘤效果，通過 IRAK4 靶向降解介導抗癌信號。

KT-474 化學結構
CAS號：2432994-31-3

KT-474 3D分子結構
CAS號：2432994-31-3

規格	價格	會員價	庫存	數量
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KT-474 純度/質量文件產品僅供科研

貨號：A1671259 標準純度： {[allProObj[0].p_purity_real_show]} 產品說明書

批次查詢：批次純度: COA SDS NMR HPLC CNMR LC-MS

全球學術期刊中引用的產品: ? Nature, 2026. Ambeed. [ A111216 , A291101 , A169647 , A115820 , A113480 , A635338 , A139877 , A258659 ]; ? Adv. Mater., 2026, e11078. Ambeed. [ A1680754 ]; ? Adv. Mater., 2026, e17774. Ambeed. [ A551995 ]; ? Cell. Mol. Immunol., 2026. Ambeed. [ A145872 , A614767 , A136097 ]; ? ACS Nano, 2026, 20(2): 2200-2210. Ambeed. [ A232266 ]; 更多 >

KT-474 生物活性

描述	KT-474是一種強效、選擇性、口服生物利用度良好的IRAK4降解劑。它通過靶向并促進IRAK4蛋白的降解，干預其在自身免疫疾病中的作用。KT-474展示了在治療包括自身免疫疾病在內的各種疾病中的潛力。
體內研究	單次口服劑量(75mg, 150mg, 300mg, 600mg, 1000mg, 1600mg)至少6天后，KT-474實現了深度和劑量依賴性的IRAK4降解。
體外研究	KT-474 在人免疫細胞中表現出對IRAK4的高選擇性降解，DC50為2.1 nM, DC90為30 nM。

KT-474 細胞實驗

Cell Line PBMCs Monocytes PBMCs PBMCs PBMCs B cells peripheral blood mononuclear cells (PBMCs)	Concentration	Treated Time	Description	References
PBMCs	200 nM	16-24 hours	To assess the degradation of IRAK4 in PBMCs. Results showed that KT-474 robustly decreased IRAK4 levels in all immune cell types.	J Invest Dermatol. 2025 Feb;145(2):323-333.e10.
Monocytes	500 nM	20 hours	To assess the effect of KT-474 on IRAK4 degradation and cytokine production in monocytes. Results showed that KT-474 decreased IRAK4 protein levels and inhibited inflammatory cytokine production.	J Invest Dermatol. 2025 Feb;145(2):323-333.e10.
PBMCs	300 nM	24 hours	To evaluate the degradation selectivity of KT-474 across the proteome. Results showed that IRAK4 was the only protein significantly downregulated.	J Med Chem. 2024 Oct 24;67(20):18022-18037.
PBMCs	300 nM	24 hours	To assess the selectivity of KT-474 in human PBMCs. Results showed that KT-474 is selective for IRAK4.	Nat Med. 2023 Dec;29(12):3127-3136.
PBMCs	1 nM (DC50), 30 nM (DC90)	24, 48, 72, 96 hours	To assess IRAK4 degradation in PBMCs. Results showed maximal degradation of IRAK4 in PBMCs is achieved by 24 hours, with sustained degradation over 96 hours (Max. degradation ~90% compared to DMSO control).	Emily Lurier etal.
B cells	0.12-2000 nM	16 hours	To assess the inhibitory effect of KT-474 on NF-κB activation in CpG-B stimulated B cells. Results showed that KT-474 inhibited NF-κB activation, whereas PF-06550833 had no effect.	Nat Med. 2023 Dec;29(12):3127-3136
peripheral blood mononuclear cells (PBMCs)	300 nM	24 hours	To evaluate the selective degradation of IRAK4 by KT-474. Results showed that KT-474 selectively degraded IRAK4 without affecting other known immune-mediated inflammatory disease substrates.	Nat Med. 2023 Dec;29(12):3127-3136

KT-474 動物實驗

Species Mice	Animal Model Imiquimod induced mouse model of psoriasis	Administration	Dosage	Frequency	Description	References
Mice	Imiquimod induced mouse model of psoriasis	Oral	30 mg/kg and 100 mg/kg	Twice a day for 3 days	To assess the anti-inflammatory efficacy of 17 in an imiquimod-induced mouse model of psoriasis. Results showed potent anti-inflammatory efficacy, comparable to topical steroid administration.	J Med Chem. 2024 Oct 24;67(20):18022-18037.

KT-474 參考文獻

[1]ACS. 2023. Discovery of KT-474, a potent, selective, and orally bioavailable IRAK4 degrader for the treatment of autoimmune diseases.

KT-474 實驗方案

計算器

存儲液制備

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.15mL

0.23mL

0.12mL

5.77mL

1.15mL

0.58mL

11.55mL

2.31mL

1.15mL

KT-474 技術信息

CAS號	2432994-31-3
分子式	C₄₄H₄₉F₂N₁₁O₆
分子量	865.93
SMILES Code	O=C1N(C=2C(=C(C#CCOC3CCN(C[C@H]4CC[C@@H](CC4)N5C=C(NC(=O)C6=C7N(N=C6)C=CC(=N7)N8[C@@]9(C[C@](C8)(OC9)[H])[H])C(C(F)F)=N5)CC3)C=CC2)N1C)C%10C(=O)NC(=O)CC%10
MDL No.	N/A

別名	PROTAC IRAK4 degrader-7; KYM-001; SAR444656; KT-I-417
運輸	藍冰

存儲條件

In solvent -20°C: 3-6個月 -80°C: 12個月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案

細胞實驗：

DMSO: 105 mg/mL(121.26 mM)，配合低頻超聲助溶，注意：DMSO長時間開封后，會吸水并導致溶解能力下降，請避免使用長期開封的DMSO

動物實驗：請根據您的動物給藥指南選擇適當的溶解方案。
以下溶解方案都請先按照體外實驗的方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議現用現配，當天使用；以下溶劑前顯示的百分比是指該溶劑在終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶

方案一

方案二

方案三

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