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

首页 / / / mTOR / XL388

XL388 {[allProObj[0].p_purity_real_show]}

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

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]}	现货	1周咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

XL388 纯度/质量文件产品仅供科研

货号：A210267 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: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 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				99%
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				98%
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。

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 细胞实验

Cell Line LN-18 cells LN-18 cells LN-18 cells LN-18 cells	Concentration	Treated Time	Description	References
LN-18 cells	300 and 1000 nM	24 hours	XL388 modestly suppressed cell growth only at the higher dose of 1,000 nM.	Int J Oncol. 2021 Oct;59(4):83
LN-18 cells	100, 500, 1000, 1500, 2000 nM	24 hours	XL388 completely inhibited phosphorylation of PRAS40 only at higher doses of 1,500 and 2,000 nM, a modest suppression was observed at 1,000 nM, and no changes in the levels of PRAS40 phosphorylation was noted at 100 and 500 nM.	Int J Oncol. 2021 Oct;59(4):83
LN-18 cells	50, 300 and 1000 nM	3 days	Treatment with XL388 failed to suppress GB cell migration at all doses as compared to the controls.	Int J Oncol. 2021 Oct;59(4):83
LN-18 cells	500 nM	4 hours	XL388 resulted in the least suppression of S‑phase entry, showing 12% of total cells in S‑phase.	Int J Oncol. 2021 Oct;59(4):83

XL388 动物实验

Species Sprague-Dawley rats	Animal Model Nerve injury-induced chronic pain model	Administration	Dosage	Frequency	Description	References
Sprague-Dawley rats	Nerve injury-induced chronic pain model	External carotid artery injection	500 nM	Single administration	To observe the effects of mTOR inhibition on brain activity in chronic pain rats, results showed that XL388 significantly reduced signal intensity in pain-related brain regions.	Mol Brain. 2020 Nov 23;13(1):158

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	455.5
SMILES Code	O=C(N1CCOC2=CC=C(C3=CC=C(N)N=C3)C=C2C1)C4=CC=C(S(=O)(C)=O)C(F)=C4C
MDL No.	MFCD24386875

别名
运输	蓝冰
InChI Key	LNFBAYSBVQBKFR-UHFFFAOYSA-N
Pubchem ID	59604787

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

XL388 {[allProObj[0].p_purity_real_show]}

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 细胞实验

XL388 动物实验

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

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

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

XL388 {[allProObj[0].p_purity_real_show]}

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 细胞实验

XL388 动物实验

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

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

XL388 纯度/质量文件产品仅供科研