ATR 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S9639 VX-803 (M4344)

VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.

Selective ATR, Ki: 150 pM
S7693 Ceralasertib (AZD6738)

AZD6738是一种口服具有活性的,选择性 ATR 激酶抑制剂,IC50 为 1 nM。Phase 1/2。

Selective ATR, IC50: 1 nM
S7050 AZ20

AZ20是一种新型有效的选择性ATR激酶抑制剂,无细胞试验中IC50为5 nM,比作用于mTOR的选择性高8倍。

Selective ATR, IC50: 5 nM
S8666 Elimusertib (BAY-1895344) hydrochloride

Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.

Selective ATR, IC50: 7 nM
S9864 Elimusertib (BAY-1895344)

Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM.

Selective ATR, IC50: 7 nM
S8050 ETP-46464

ETP-46464是一种有效的,选择性ATR抑制剂,IC50为25 nM。

Selective ATR, IC50: 14 nM
S7102 Berzosertib (VE-822)

VE-822是一种ATR抑制剂,在HT29细胞中IC50 为 19 nM。

Selective ATR, IC50: 19 nM
S1009 Dactolisib (BEZ235)

Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3KmTOR 抑制剂,在无细胞试验中,抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR,IC50 为 21 nM,而对 Akt 和 PDK1 的抑制作用很弱。Phase 2。

Selective ATR, IC50: 21 nM
S8007 VE-821

VE-821是一种有效的,选择性的,ATP竞争性ATR抑制剂,在无细胞试验中Ki/IC50为13 nM/26 nM,抑制H2AX磷酸化,对PIKKs ATM, DNA-PK, mTOR和PI3Kγ具有很低的抑制活性。

Selective ATR, Ki: 13 nM
S3600 Schisandrin B (Sch B)

Schisandrin B (Sch B)是中草药五味子(Turcz.)中含量最丰富的二苯并环辛二烯木酚素。它是一种安全的ATRP-gp抑制剂。

Selective ATR, IC50: 7.25 μM
S0148 HAMNO

HAMNO is a novel replication protein A (RPA) inhibitor that inhibits protein interaction.

Selective
S2817 Torin 2

Torin 2 是一种有效的选择性mTOR抑制剂,在p53−/− MEFs细胞系中IC50为0.25 nM;作用于mTOR比作用于PI3K选择性高800倍,并且改善了药代动力学性能。抑制ATM/ATR/DNA-PK,在PC3细胞系中EC50分别为28 nM/35 nM/118 nM。

Pan ATR, EC50: 35 nM
S7136 CGK 733

CGK 733是一种有效的ATM/ATR选择性抑制剂,IC50约为200 nM。

Pan ATR, IC50: 200 nM