XL388 | mTOR Inhibitor | AmBeed-信号通路专用抑制剂

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XL388 99%+

货号：A210267

XL388 is a potent and selective ATP-competitive mTOR inhibitor with IC50 value of 9.9 nM.

XL388 化学结构
CAS号：1251156-08-7

XL388 3D分子结构
CAS号：1251156-08-7

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XL388 纯度/质量文件产品仅供科研

货号：A210267 标准纯度： 99%+ 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: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

mTOR 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				99%
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。

XL388 生物活性

靶点	mTORC1 mTORC1, IC50:8 nM mTORC2 mTORC2, IC50:166 nM mTOR mTOR, IC50:9.9 nM
描述	The mammalian target of rapamycin (mTOR) is a large protein kinase that integrates both extracellular and intracellular signals of cellular growth, proliferation, and survival, which lies in two different multi-protein complexes, including mTOR complex 1(mTORC1) and mTORC2. XL388 is an orally bioavailable inhibitor of the mTOR that inhibits cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates, with IC₅₀ value of 9.9 nM^[4]. XL388(5-200nM)-treated MG-63 cells showed increased percentage of G1 phase and decreased S phase and G2-M phase compared with untreated cells. Oral administration of XL388 (20 mg/kg body weight, every three days, × 7 times) significantly inhibited human osteosarcoma cell line U2OS xenograft growth in severe combined immuno-defcient mice more than 40%^[5]. XL388 (10-1000 nM, 24-96 h) dose- and time-dependently induced renal cell carcinoma cell line 786-0 cell death. Consistently, oral administration of XL388 (20 mg/kg, every three days, × 7 times) dramatically inhibited 786-0 tumor growth in nude mice more than 60%^[6].
作用机制	XL388 inhibits mTOR activity in an ATP-competitive manner.

XL388 动物研究

Dose

Mice: 20 mg/kg^[2] (p.o.); 10 mg/kg^[1] (i.v.); 50 mg/kg^[3] (i.p.) Rat: 3 mg/kg^[1] (i.v./p.o.) Dog: 3 mg/kg^[1] (i.v./p.o.)

Administration

p.o., i.v.

Pharmacokinetics

Animal	Mice^[1]	Rats^[1]	Dogs^[1]	Monkeys^[1]
Dose	10 mg/kg	3 mg/kg	3 mg/kg	3 mg/kg
Administration	i.v. or p.o.	i.v. or p.o.	i.v. or p.o.	i.v. or p.o.
F	31.4% (p.o.)	25.6% (p.o.)	69.6% (p.o.)	53.4% (p.o.)
T_1/2	1.35 h (i.v.)	0.45 h (i.v.)	0.45 h (i.v.)	0.86 h (i.v.)
T_max	0.5 h (p.o.)	0.5 h (p.o.)	6.11 h (p.o.)	2.0 h (p.o.)
CL	2.75 L/kg/h (i.v.)	1.27 L/kg/h (i.v.)	0.598 L/kg/h (i.v.)	5.05 L/kg/h (i.v.)
C_max	9.14 μM (i.v.) 1.30 μM (p.o.)	4.12 μM (i.v.) 0.707 μM (p.o.)	2.28 μM (i.v.) 1.66 μM (p.o.)	0.95 μM (i.v.) 0.25 μM (p.o.)
AUC_0→∞	8.00 μM·h (i.v.) 2.51 μM·h (p.o.)	3.72 μM·h (i.v.) 0.952 μM·h (p.o.)	11.0 μM·h (i.v.) 7.66 μM·h (p.o.)	1.31 μM·h (i.v.) 0.70 μM·h (p.o.)
Vss	1.96 L/kg (i.v.)	1.27 L/kg (i.v.)	3.15 L/kg (i.v.)	6.42 L/kg (i.v.)

XL388 参考文献

[1]Takeuchi CS, Kim BG, et al. Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR). J Med Chem. 2013 Mar 28;56(6):2218-34.

[2]Zhu YR, Zhou XZ, et al. The anti-cancer activity of the mTORC1/2 dual inhibitor XL388 in preclinical osteosarcoma models. Oncotarget. 2016 Aug 2;7(31):49527-49538.

[3]Yu K, Toral-Barza L, et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 2009 Aug 1;69(15):6232-40.

[4]Takeuchi CS, Kim BG, Blazey CM, Ma S, Johnson HW, Anand NK, Arcalas A, Baik TG, Buhr CA, Cannoy J, Epshteyn S, Joshi A, Lara K, Lee MS, Wang L, Leahy JW, Nuss JM, Aay N, Aoyama R, Foster P, Lee J, Lehoux I, Munagala N, Plonowski A, Rajan S, Woolfrey J, Yamaguchi K, Lamb P, Miller N. Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR). J Med Chem. 2013 Mar 28;56(6):2218-34. doi: 10.1021/jm3007933. Epub 2013 Mar 7. PMID: 23394126.

[5]Zhu YR, Zhou XZ, Zhu LQ, Yao C, Fang JF, Zhou F, Deng XW, Zhang YQ. The anti-cancer activity of the mTORC1/2 dual inhibitor XL388 in preclinical osteosarcoma models. Oncotarget. 2016 Aug 2;7(31):49527-49538. doi: 10.18632/oncotarget.10389. PMID: 27385099; PMCID: PMC5226526.

[6]Xiong Z, Zang Y, Zhong S, Zou L, Wu Y, Liu S, Fang Z, Shen Z, Ding Q, Chen S. The preclinical assessment of XL388, a mTOR kinase inhibitor, as a promising anti-renal cell carcinoma agent. Oncotarget. 2017 May 2;8(18):30151-30161. doi: 10.18632/oncotarget.15620. PMID: 28404914; PMCID: PMC5444733.

XL388 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

10.98mL

2.20mL

1.10mL

21.95mL

4.39mL

2.20mL

XL388 技术信息

CAS号	1251156-08-7
分子式	C₂₃H₂₂FN₃O₄S
分子量	455.502

别名
运输	蓝冰

存储条件

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

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(109.77 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

30% PEG400+0.5% Tween80+5% propylene glycol+water 30 mg/mL suspension

XL388 99%+

XL388 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

XL388 质控信息

XL388 生物活性

XL388 动物研究

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XL388 实验方案

XL388 技术信息

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mTORC1	mTORC1, IC50:8 nM
mTORC2	mTORC2, IC50:166 nM
mTOR	mTOR, IC50:9.9 nM

XL388 99%+

XL388 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

XL388 质控信息

XL388 生物活性

XL388 动物研究

XL388 参考文献

XL388 实验方案

XL388 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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