CZ415 | mTOR Inhibitor | AmBeed-信号通路专用抑制剂

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CZ415 {[allProObj[0].p_purity_real_show]}

货号：A569091

CZ415 is a potent and highly selective ATP-competitive mTOR inhibitor with pKd^app value of 8.2.

CZ415 化学结构
CAS号：1429639-50-8

CZ415 3D分子结构
CAS号：1429639-50-8

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CZ415 纯度/质量文件产品仅供科研

货号：A569091 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

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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			PDGFR,DNA-PK	99%+
Everolimus					99%+
WYE-354	+++ mTOR, IC50: 5 nM				98%
Tacrolimus	✔				98%
PP121	++ mTOR, IC50: 13 nM			PDGFR,VEGFR	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。

CZ415 生物活性

靶点	mTOR mTOR, pIC50:8.07
描述	The mammalian target of rapamycin (mTOR/FRAP1) is a serine/threonine protein kinase, which belongs to a family of phosphoinositide 3-kinase-related kinases (PIKK). mTOR is the catalytic subunit of two signaling complexes called mTORC1 and mTORC2, which play a critical role in regulation of cell metabolism, proliferation, survival and migration. CZ415 is a potent and highly selective ATP-competitive mTOR inhibitor with Kd^app value of 6.9 nM, and shows efficacy in a semi-therapeutic collagen induced arthritis (CIA) mouse model^[3]. CZ514 (1-1000 nM) dose-dependently inhibited human papillary thyroid carcinoma cell line TPC-1 cell growth, induced cleavage of both caspase-3 and caspase-9 and disrupted cycle progression. Consistently, oral administration of CZ415 (20 mg/kg body weight, daily for 24 days) significantly reduced TPC-1 xenograft tumor volume in mice more than 60%^[4]. CZ415 dose-dependently inhibited HepG2 cell survival with IC₅₀ of 233.75 ±22.54 nM. HepG2 tumor growth in SCID mice was decreased to 13.93 ± 3.72 mm³ after oral administration of CZ415 (10 mg/kg body weight, daily), compared with 43.52 ± 4.5 mm³ in vehicle control mice^[5]. It was also found that CZ415 (from 1 to 300 nM) dose-dependently inhibited head and neck squamous cell carcinoma cell line SCC-9 survival^[6].
作用机制	CZ415 inhibits mTOR activity in an ATP-competitive manner.

CZ415 动物研究

Dose

Rat: 1 mg/kg^[1] (i.v.); 3 mg/kg^[1] (p.o.) Mice: 1 mg/kg - 10 mg/kg^[1] (p.o., BID), 25 mg/kg^[2] (0.g.)

Administration

i.v., p.o., o.g.

Pharmacokinetics

Animal	Rats^[1]
Dose	1 mg/kg (i.v.) 3 mg/kg (p.o.)
Administration	i.v. p.o.
MRT	1.1 h
F	44% (p.o.)
AUC_0-inf	0.76 μM·h (i.v.) 1.0 μM·h (p.o.)
CL_p	49 ml/min/kg (i.v.)
CL_b	41 ml/min/kg (i.v.)
C_max	0.71 μM (i.v.) 0.43 μM (p.o.)
Vd_ss	3.1 L/kg (i.v.)

CZ415 参考文献

[1]Cansfield AD, Ladduwahetty T, et al. CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model. ACS Med Chem Lett. 2016 Jun 10;7(8):768-73.

[2]Yin G, Fan J, et al. ERK inhibition sensitizes CZ415-induced anti-osteosarcoma activity in vitro and in vivo. Oncotarget. 2017 May 30;8(47):82027-82036.

[3]Cansfield AD, Ladduwahetty T, Sunose M, Ellard K, Lynch R, Newton AL, Lewis A, Bennett G, Zinn N, Thomson DW, Rüger AJ, Feutrill JT, Rausch O, Watt AP, Bergamini G. CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model. ACS Med Chem Lett. 2016 Jun 10;7(8):768-73. doi: 10.1021/acsmedchemlett.6b00149. PMID: 27563401; PMCID: PMC4983736.

[4]Li X, Li Z, Song Y, Liu W, Liu Z. The mTOR Kinase Inhibitor CZ415 Inhibits Human Papillary Thyroid Carcinoma Cell Growth. Cell Physiol Biochem. 2018;46(2):579-590. doi: 10.1159/000488625. Epub 2018 Mar 28. PMID: 29617677.

[5]Zhang W, Chen B, Zhang Y, Li K, Hao K, Jiang L, Wang Y, Mou X, Xu X, Wang Z. The anti-hepatocellular carcinoma cell activity by a novel mTOR kinase inhibitor CZ415. Biochem Biophys Res Commun. 2017 Jun 3;487(3):494-499. doi: 10.1016/j.bbrc.2017.03.156. Epub 2017 Mar 30. PMID: 28366631.

[6]Xie J, Li Q, Ding X, Gao Y. Targeting mTOR by CZ415 Inhibits Head and Neck Squamous Cell Carcinoma Cells. Cell Physiol Biochem. 2018;46(2):676-686. doi: 10.1159/000488724. Epub 2018 Mar 29. PMID: 29621758.

CZ415 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.88mL

2.18mL

1.09mL

21.76mL

4.35mL

2.18mL

CZ415 技术信息

CAS号	1429639-50-8
分子式	C₂₂H₂₉N₅O₄S
分子量	459.562

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 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(228.48 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

CZ415 {[allProObj[0].p_purity_real_show]}

CZ415 纯度/质量文件产品仅供科研

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CZ415 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

CZ415 质控信息

CZ415 生物活性

CZ415 动物研究

CZ415 参考文献

CZ415 实验方案

CZ415 技术信息

最近浏览的产品

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摩尔计算器

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总药量计算器

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