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

CZ415 {[allProObj[0].p_purity_real_show]}

货号：A569091

CZ415是一种强效且高度选择性的ATP竞争性mTOR抑制剂，pKd^app值为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 质控信息

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。

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 细胞实验

Cell Line Human whole blood cells HEK293T cells Primary human OS cells (primary OS2) Primary human OS cells (primary OS1) SaOs2 cells MG-63 cells U2OS cells	Concentration	Treated Time	Description	References
Human whole blood cells	226 nM IC50	18 hours	Inhibition of IFNγ release	ACS Med Chem Lett. 2016 Jun 10;7(8):768-73.
HEK293T cells	14.5 nM IC50	2 hours	Inhibition of S6RP phosphorylation	ACS Med Chem Lett. 2016 Jun 10;7(8):768-73.
Primary human OS cells (primary OS2)	25/100 nM		CZ415 inhibited survival of primary human OS cells (primary OS2)	Oncotarget. 2017 May 30;8(47):82027-82036.
Primary human OS cells (primary OS1)	25/100 nM		CZ415 inhibited survival of primary human OS cells (primary OS1)	Oncotarget. 2017 May 30;8(47):82027-82036.
SaOs2 cells	25-1000 nM	72 hours	CZ415 concentration-dependently inhibited survival of SaOs2 cells	Oncotarget. 2017 May 30;8(47):82027-82036.
MG-63 cells	25-1000 nM	72 hours	CZ415 concentration-dependently inhibited survival of MG-63 cells	Oncotarget. 2017 May 30;8(47):82027-82036.
U2OS cells	25-1000 nM	72 hours	CZ415 concentration-dependently inhibited survival of U2OS cells	Oncotarget. 2017 May 30;8(47):82027-82036.

Cell Line

Human whole blood cells HEK293T cells Primary human OS cells (primary OS2) Primary human OS cells (primary OS1) SaOs2 cells MG-63 cells U2OS cells

Concentration

Treated Time

Description

References

Human whole blood cells

226 nM IC50

18 hours

Inhibition of IFNγ release

ACS Med Chem Lett. 2016 Jun 10;7(8):768-73.

HEK293T cells

14.5 nM IC50

2 hours

Inhibition of S6RP phosphorylation

ACS Med Chem Lett. 2016 Jun 10;7(8):768-73.

Primary human OS cells (primary OS2)

25/100 nM

CZ415 inhibited survival of primary human OS cells (primary OS2)

Oncotarget. 2017 May 30;8(47):82027-82036.

Primary human OS cells (primary OS1)

25/100 nM

CZ415 inhibited survival of primary human OS cells (primary OS1)

Oncotarget. 2017 May 30;8(47):82027-82036.

SaOs2 cells

25-1000 nM

72 hours

CZ415 concentration-dependently inhibited survival of SaOs2 cells

Oncotarget. 2017 May 30;8(47):82027-82036.

MG-63 cells

25-1000 nM

72 hours

CZ415 concentration-dependently inhibited survival of MG-63 cells

Oncotarget. 2017 May 30;8(47):82027-82036.

U2OS cells

25-1000 nM

72 hours

CZ415 concentration-dependently inhibited survival of U2OS cells

Oncotarget. 2017 May 30;8(47):82027-82036.

CZ415 动物实验

Species Mice SCID mice	Animal Model Anti-CD3 mouse model U2OS tumor xenograft model	Administration	Dosage	Frequency	Description	References
Mice	Anti-CD3 mouse model	Oral	1, 3, and 10 mg/kg	1 hour before stimulus	Inhibition of mTOR downstream signaling	ACS Med Chem Lett. 2016 Jun 10;7(8):768-73.
SCID mice	U2OS tumor xenograft model	Oral	25 mg/kg	Daily for 21 days	CZ415 oral administration efficiently inhibited U2OS tumor growth in mice, and its activity was further potentiated with co-administration of MEK162	Oncotarget. 2017 May 30;8(47):82027-82036.

Species

Mice SCID mice

Animal Model

Anti-CD3 mouse model U2OS tumor xenograft model

Administration

Dosage

Frequency

Description

References

Mice

Anti-CD3 mouse model

Oral

1, 3, and 10 mg/kg

1 hour before stimulus

Inhibition of mTOR downstream signaling

ACS Med Chem Lett. 2016 Jun 10;7(8):768-73.

SCID mice

U2OS tumor xenograft model

Oral

25 mg/kg

Daily for 21 days

CZ415 oral administration efficiently inhibited U2OS tumor growth in mice, and its activity was further potentiated with co-administration of MEK162

Oncotarget. 2017 May 30;8(47):82027-82036.

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

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	459.56
SMILES Code	O=C(NCC)NC1=CC=C(C2=NC(N3[C@@H](C)COCC3)=C4C(C(C)(C)S(C4)(=O)=O)=N2)C=C1
MDL No.	MFCD30533321

别名
运输	蓝冰
InChI Key	IZLPVLBNRGPOHA-AWEZNQCLSA-N
Pubchem ID	71547699

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

细胞实验：

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：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

方案三

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