T025 | CLK Inhibitor | AmBeed-信号通路专用抑制剂

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T025 {[allProObj[0].p_purity_real_show]}

货号：A1365253

T025是一种具有口服活性的 Cdc2-like 激酶 (CLK) 抑制剂，对多种 CLK 激酶亚型的 Kd 值在纳摩尔级别 (如 CLK2 为 0.096 nM)。T025 可诱导 caspase-3/7 介导的细胞凋亡，适用于 MYC 驱动的肿瘤和细胞增殖异常的疾病研究。

T025 化学结构
CAS号：2407433-00-3

T025 3D分子结构
CAS号：2407433-00-3

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T025 纯度/质量文件产品仅供科研

货号：A1365253 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

mTOR 亚型比较
DYRK 亚型比较
CDK 亚型比较

产品名称	mTOR ↓ ↑	mTORC1 ↓ ↑	mTORC2 ↓ ↑	其他靶点	纯度
AZD-8055	++++ mTOR (full length), IC50: 0.8 nM mTOR (truncated), IC50: 0.13 nM				99%+
Gedatolisib	++++ mTOR, IC50: 1.6 nM				98%
GSK1059615	++ mTOR, IC50: 12 nM				98%
Vistusertib	+++ mTOR, IC50: 2.8 nM				99%+
Torin 1	+++ mTOR, IC50: 4.32 nM	+++ mTORC1, IC50: 2 nM	++ mTORC2, IC50: 10 nM	DNA-PK	99%+
Dactolisib	+++ mTOR (p70S6K), IC50: 6 nM				98+%
PI-103	+ mTOR, IC50: 30 nM				99%+
WAY-600	++ mTOR, IC50: 9 nM				99%
Voxtalisib	+ mTOR, IC50: 157 nM				99%+
PF-04691502	++ mTOR, Ki: 16 nM				98+%
Onatasertib	++ mTOR, IC50: 16 nM			DNA-PK	99%+
Chrysophanol	✔			EGFR	98%
Samotolisib	✔			DNA-PK	99%+
Torkinib	+++ mTOR, IC50: 8 nM			DNA-PK,PDGFR	99%+
Everolimus					99%+
WYE-354	+++ mTOR, IC50: 5 nM				98%
Tacrolimus	✔				98%
PP121	++ mTOR, IC50: 13 nM			VEGFR,PDGFR	99%+
Torin 2	++++ mTOR, IC50: 0.25 nM			DNA-PK	99%+
Rapamycin	++++ mTOR, IC50: ~0.1 nM				98%
GDC-0349	+++ mTOR, Ki: 3.8 nM				98%
XL388	++ mTOR, IC50: 9.9 nM	+++ mTORC1, IC50: 8 nM	+ mTORC2, IC50: 166 nM		99%+
WYE-687	+++ mTOR, IC50: 7 nM				98+%
Apitolisib	+ mTOR, Ki app: 17 nM				98%+
WYE-132	++++ mTOR, IC50: 0.19 nM				99%+
Sapanisertib	++++ mTOR, Ki: 1.4 nM				99%+
BGT226 maleate	✔				99%+
ETP-46464	++++ mTOR, IC50: 0.6 nM			DNA-PK	98%
PI3K-IN-1	+ mTOR, IC50: 157 nM				98+%
Zotarolimus	+++ FKBP-12, IC50: 2.8 nM				99+%
OSI-027	+++ mTOR, IC50: 4 nM	+ mTORC1, IC50: 22 nM	+ mTORC2, IC50: 65 nM		99%+
Ridaforolimus	++++ mTOR, IC50: 0.2 nM				99%+
Temsirolimus	+ mTOR, IC50: 1.76 μM				95%
CZ415	++ mTOR, pIC50: 8.07				99%+
SF2523	+ mTOR, IC50: 280 nM			DNA-PK	99%+
KU-0063794		++ mTORC1, IC50: ~10 nM	++ mTORC2, IC50: ~10 nM		99%+
Omipalisib		++++ mTORC1, Ki: 0.18 nM	++++ mTORC2, Ki: 0.3 nM		99%+
Palomid 529		✔			99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	DYRK ↓ ↑	DYRK1 ↓ ↑	DYRK2 ↓ ↑	纯度
ID-8	✔			99%+
AZ191		++++ DYRK1B, IC50: 17 nM DYRK1A, IC50: 88 nM		98%
Harmine		+++ DYRK1B, IC50: 166 nM DYRK1A, IC50: 33 nM	++ DYRK2, IC50: 1.9 μM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 hydrochloride	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											ERK,SGK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	98%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinE, IC50: 8 nM CDK2/CyclinA, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	98%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 dihydrochloride									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				98+%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			99+%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

T025 生物活性

描述

T025 is a potent, orally active inhibitor of Cdc2-like kinases (CLKs) with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5, and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B, and DYRK2, respectively. T025 induced caspase-3/7-mediated apoptosis in MDA-MB-468 cells at concentrations of 0, 10, 30, 100, 300 and 1000 nM for 6 h. T025 exhibited antiproliferative activity in both haematological and solid cancer cell lines tested (IC50 values: 30-300 nM). It has antitumour efficacy and is mainly used in MYC-driven disease studies^[1].

T025 动物研究

Animal study

When administered orally at a dose of 50 mg/kg twice a day, 2 days a week for 3 weeks, T025 inhibited the growth of MDA-MB-468 xenografts and decreased body weight by less than 10% in Balb/c nude mice^[1].

T025 参考文献

[1]Iwai K, et al. Anti-tumor efficacy of a novel CLK inhibitor via targeting RNA splicing and MYC-dependent vulnerability. EMBO Mol Med. 2018 Jun;10(6):e8289.

T025 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.07mL

2.61mL

1.31mL

26.15mL

5.23mL

2.61mL

T025 技术信息

CAS号	2407433-00-3
分子式	C₂₁H₁₈N₈
分子量	382.421

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 7 mg/mL(18.3 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

T025 {[allProObj[0].p_purity_real_show]}

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