PP121 | mTOR Inhibitor | AmBeed-信号通路专用抑制剂

PP121 {[allProObj[0].p_purity_real_show]}

货号：A986976

PP121是一种多靶向抑制剂，能够抑制 PDGFR、Hck、mTOR、VEGFR2、Src 和 Abl，IC50 分别为 2 nM、8 nM、10 nM、12 nM、14 nM 和 18 nM，同时还能抑制 DNA-PK，IC50 为 60 nM。

PP121 化学结构
CAS号：1092788-83-4

PP121 3D分子结构
CAS号：1092788-83-4

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mTOR 亚型比较

PDGFR 亚型比较

VEGFR 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			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				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。

产品名称	PDGFR ↓ ↑	PDGFRα ↓ ↑	PDGFRβ ↓ ↑	其他靶点	纯度
Tyrphostin A9	+ PDGFR, IC50: 0.5 μM			EGFR	98%
Tyrphostin AG1296					99%+
Motesanib Diphosphate	++ PDGFR, IC50: 84 nM				97%
Pazopanib	++ PDGFR, IC50: 84 nM				99%
Imatinib	+ PDGFR, IC50: 100 nM			c-Kit	98%
Imatinib Mesylate	+ PDGFR, IC50: 100 nM			c-Kit	99%
Sennoside B	✔				99%+
PP121	++++ PDGFR, IC50: 2 nM			VEGFR,mTOR	99%+
Crenolanib		++++ PDGFRα, Kd: 2.1 nM	++++ PDGFRβ, Kd: 3.2 nM		99%+
Masitinib		+ PDGFRα, IC50: 540 nM	+ PDGFRβ, IC50: 800 nM		99%+
Ki8751		++ PDGFRα, IC50: 67 nM		c-Kit	99%
Tivozanib		++ PDGFRα, IC50: 40 nM	++ PDGFRβ, IC50: 49 nM		99%+
Ponatinib		++++ PDGFRα, IC50: 1.1 nM			98%
Amuvatinib		++ PDGFRα (V561D), IC50: 40 nM			99%+
Axitinib		+++ PDGFRα, IC50: 5.0 nM	++++ PDGFRβ, IC50: 1.6 nM		98%
CP-673451		+++ PDGFRα, IC50: 10 nM	++++ PDGFRβ, IC50: 1 nM		99%+
Telatinib		+++ PDGFRα, IC50: 15 nM		c-Kit	99%+
Nintedanib		++ PDGFRα, IC50: 59 nM	++ PDGFRβ, IC50: 65 nM		99+%
Avapritinib		++++ PDGFRα (D842V), IC50: 0.5 nM			99%+
MK-2461			+++ PDGFRβ, IC50: 22 nM		98%+
Lactate			+++ PDGFRβ, IC50: 27 nM	c-Kit,FLT3	85%
Linifanib			++ PDGFRβ, IC50: 66 nM		99%+
AZD2932			+++ PDGFRβ, IC50: 4 nM	c-Kit	99%
Dovitinib			+++ PDGFRβ, IC50: 27 nM	c-Kit,FLT3	99%+
Sorafenib			++ PDGFRβ, IC50: 57 nM mPDGFRβ, IC50: 57 nM		99%
Sunitinib			++++ PDGFRβ , IC50: 2 nM	FLT3	98%
Orantinib			+++ PDGFRβ, Ki: 8 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。

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2/Flk1, IC50: 3 nM VEGFR2, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	PDGFR,RET	97%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ Flk1, IC50: 25 nM VEGFR2, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	FGFR,PDGFR,c-Kit	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/Flk1, IC50: 270 nM VEGFR2/KDR, IC50: 37 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Kit,c-Fms/CSF1R	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/Flk1, IC50: 0.18 nM VEGFR2/KDR, IC50: 0.2 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	BTK,c-Kit	98%
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ mVEGF2, IC50: 165 nM hVEGFR2, IC50: 9 nM	+ hVEGFR3, IC50: 420 nM		99%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			99%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	99%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Apatinib mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	99%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2/Flk1, IC50: 90 nM VEGFR2, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	99%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	RET,FLT3	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	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。

PP121 生物活性

靶点

mTOR

mTOR, IC50:13 nM
DNA-PK

DNA-PK, IC50:60 nM
PDGFR

PDGFR, IC50:2 nM
Src

Src, IC50:14 nM
Abl

Abl, IC50:18 nM

描述

PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.

PP121 细胞实验

Cell Line Tyk-nu-GFP NIH3T3 cells BaF3 cells K562 cells TT thyroid carcinoma cells LN229 cells U87 cells Mouse tracheal rings (mTRs) Human bronchial epithelial cells (16HBE) Non-small cell lung cancer cells (NCI-H2170) Non-small cell lung cancer cells (NCI-H1975)	Concentration	Treated Time	Description	References
Tyk-nu-GFP	5μM	72 hours	Inhibited ovarian cancer cell proliferation	Mol Cancer Ther. 2020 Jan;19(1):52-62.
NIH3T3 cells	2.5 µM	2 h	PP121 blocked tyrosine phosphorylation induced by v-Src and restored actin stress fiber staining.	Nat Chem Biol. 2008 Nov;4(11):691-9.
BaF3 cells	0.080 to 20 µM	120 min	PP121 inhibited Bcr-Abl induced tyrosine phosphorylation in BaF3 cells.	Nat Chem Biol. 2008 Nov;4(11):691-9.
K562 cells	0.080 to 20 µM	120 min	PP121 inhibited Bcr-Abl induced tyrosine phosphorylation in K562 cells.	Nat Chem Biol. 2008 Nov;4(11):691-9.
TT thyroid carcinoma cells	0.040 to 10 µM	2 h	PP121 inhibited Ret autophosphorylation in cells at low nanomolar concentrations.	Nat Chem Biol. 2008 Nov;4(11):691-9.
LN229 cells	0.040 to 10 µM		PP121 inhibited the phosphorylation of Akt, p70S6K and S6 in these cells, but had no effect on the phosphorylation of Erk at concentrations up to 10 µM.	Nat Chem Biol. 2008 Nov;4(11):691-9.
U87 cells	0.040 to 10 µM		PP121 inhibited the phosphorylation of Akt, p70S6K and S6 in these cells, but had no effect on the phosphorylation of Erk at concentrations up to 10 µM.	Nat Chem Biol. 2008 Nov;4(11):691-9.
Mouse tracheal rings (mTRs)	4.19 ± 0.06 µM (IC50), 14.98 ± 0.06 µM (IC75)		PP121 relaxed precontracted mouse tracheal rings by blocking certain ion channels, including L-type voltage-dependent Ca2+ channels (L-VDCCs), nonselective cation channels (NSCCs), transient receptor potential channels (TRPCs), Na+/Ca2+ exchangers (NCXs) and K+ channels, and accelerating calcium mobilization.	Mol Med. 2023 Nov 7;29(1):154.
Human bronchial epithelial cells (16HBE)	3.16 µM, 10 µM, 56.23 µM	24 hours or 48 hours	PP121 had no effect on the viability of 16HBE cells at low (3.16 µM) and medium (10 µM) concentrations, but inhibited cell viability at high concentration (56.23 µM) after 48 hours.	Mol Med. 2023 Nov 7;29(1):154.
Non-small cell lung cancer cells (NCI-H2170)	500 nM-10 µM	48 hours	To evaluate the inhibitory effect of PP121 on the proliferation of non-small cell lung cancer cells, results showed that PP121 decreased cell viability in a dose-dependent manner.	Biomed Rep. 2023 Mar 1;18(4):29.
Non-small cell lung cancer cells (NCI-H1975)	500 nM-10 µM	48 hours	To evaluate the inhibitory effect of PP121 on the proliferation of non-small cell lung cancer cells, results showed that PP121 decreased cell viability in a dose-dependent manner.	Biomed Rep. 2023 Mar 1;18(4):29.

Cell Line

Concentration

Treated Time

Description

References

Tyk-nu-GFP

5μM

72 hours

Inhibited ovarian cancer cell proliferation

Mol Cancer Ther. 2020 Jan;19(1):52-62.

NIH3T3 cells

2.5 µM

2 h

PP121 blocked tyrosine phosphorylation induced by v-Src and restored actin stress fiber staining.