|2-(4-氨基-1-异丙基-1H-吡唑并[3,4-d]嘧啶-3-基)-1H-吲哚-5-醇|CsnPharm

CAS No.: 1092351-67-1

Torkinib Catalog No. CSN12732

Synonyms: PP 242

PP 242 is the first selective and ATP competitive mTOR inhibitor with IC50 of 8 nM.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Bromodomain 4

Kd:1.7μM mTOR

IC50:8nM p110δ

IC50:100nM
描述Phosphoinositide 3-kinase (PI3-K) family members include p110α that is the most frequently mutated kinase in human cancer, and mTOR, which is a central regulator of cell growth and some other enzymes. PP242 exhibits potent selectivity for mTOR with IC50 of 8nM over other PI3K family kinases like p110α, p110β, p110γ, p110δ and DNA-PK with IC50 of 1.96μM, 2.2μM, 1.27μM, 0.102μM, and 0.408μM, respectively. In BT549 cells, PP242 treatment with concentration range 0.04-10μM inhibited the phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6 in a dose-dependent manner. PP242 potently inhibits PKCα with IC50 of 49nM. Low concentrations of PP242 inhibited the phosphorylation of Akt at S473 site, confirming that mTOR kinase activity was required for hydrophobic motif phosphorylation. Higher concentrations partially inhibited Akt T308-P in addition to S473-P, the effect of which on the phosphorylation of Akt in primary MEFs from embryos that lacked SIN1. PP242 was more effective to inhibit mTORC1 and inhibited the proliferation of primary MEFs, and the phosphorylation of 4EBP1 at T36/45 and S65. PP242 potently inhibited cap-dependent translation, by causing a higher level of binding between 4EBP1 and eIF4E, suggesting that cap-dependent translation will be more highly suppressed by PP242. After 8 h of treatment with PP242, no obvious effect on the morphology or abundance of actin stress fibers was found. Besides, PP242 had a dose-dependent effect on proliferation and at higher doses was much more effective at blocking cell proliferation. PP242 potently inhibited the proliferation of p190-transformed murine BM, SUP-B15, and K562 cells with GI50 of 12nM (cell growth was suppressed by 90%), 90 nM, and 85 nM, respectively, as well as inhibited the growth of solid tumor cell lines such as SKOV3 and U87 with GI50 of 0.49μM and 1.57μM, respectively. In adaptive immune function assays, PP242 had little effect at 1–10nM. While with increasing effects at 100nM and 1µM, the latter far exceeding its effective concentration for inhibiting growth in leukemia cell lines which also decreased the size of activated T cells.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
3T3-L1	15 μM	Function Assay	4 h	suppresses expression of the Egr1 protein	25814662
786-O	0.1/0.5 μM	Function Assay	24 h	increases E-cadherin mRNA levels dose dependently	23147251
786-O	0-0.5 μM	Function Assay	24 h	results in a dose dependent increase in E-cadherin protein expression	23147251

更多
动物研究
剂量
Mice: 60 mg/kg^[3] (p.o.), 100 mg/kg^[4] (p.o.), 30 mg/kg^[5] (i.p.) Nude Mice: 200 mg/kg^[6] (p.o.) Rat: 15 mg/kg^[7] (i.p.)

给药途径
p.o., i.p.

动物研究
剂量	Mice: 60 mg/kg^[3] (p.o.), 100 mg/kg^[4] (p.o.), 30 mg/kg^[5] (i.p.) Nude Mice: 200 mg/kg^[6] (p.o.) Rat: 15 mg/kg^[7] (i.p.)
给药途径	p.o., i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2432 mL
- 16.2160 mL
- 32.4320 mL
- 5 mM
- 0.6486 mL
- 3.2432 mL
- 6.4864 mL
- 10 mM
- 0.3243 mL
- 1.6216 mL
- 3.2432 mL

技术信息

CAS号

1092351-67-1

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H16N6O

运输

蓝冰

分子量

308.34

别名

PP 242

溶解度

DMSO	500.0 mg/mL (1621.6 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	10 mg/mL	clear
PO	0.5% CMC-Na	34 mg/mL	suspension

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

3T3-L1	15 μM	Function Assay	4 h	suppresses expression of the Egr1 protein	25814662
786-O	0.1/0.5 μM	Function Assay	24 h	increases E-cadherin mRNA levels dose dependently	23147251
786-O	0-0.5 μM	Function Assay	24 h	results in a dose dependent increase in E-cadherin protein expression	23147251
8226	100-1000 nM	Function Assay	30 min	activates ERK	22556409
8226	0.5 μM	Function Assay	30 min	induces activation of RAF and phosphorylation of MEK	22556409
AGS	0-1000 nM	Cell Viability Assay	24/48 h	decreases cell viability in time and dose dependent manner	25035961
BaF3	-	Growth Inhibition Assay	-	GI50=1.449 μM	22223645
Bcap-37	50/200/500 nM	Function Assay	30 min	dose-dependently (50–500 nM) suppresses phosphorylation of Akt	22476852
Bcap-37	200 nM	Apoptosis Assay	36 h	induces apoptosis	22476852
Caco2	0-1000 nM	Cell Viability Assay	24 h	inhibits the growth in a dose-dependent manner	23991179
Caco-2	-	Growth Inhibition Assay	-	IC50=0.22 μM	23542178
COLO 201	-	Growth Inhibition Assay	-	IC50=0.23 μM	23542178
COLO 205	-	Growth Inhibition Assay	-	IC50=0.24 μM	23542178
Colo205	0-1000 nM	Cell Viability Assay	24 h	inhibits the growth in a dose-dependent manner	23991179
Colo320	0-1000 nM	Cell Viability Assay	24 h	inhibits the growth in a dose-dependent manner	23991179
Colo320	1 μM	Function Assay	0-24 h	abolishes the S6S235/236 but partially reduces the 4E-BP1T36/45	23991179
DLD-1	0-1000 nM	Cell Viability Assay	24 h	inhibits the growth in a dose-dependent manner	23991179
DLD-1	1 μM	Function Assay	0-24 h	abolishes the S6S235/236 but partially reduces the 4E-BP1T36/45	23991179
DLD-1	10/100/1000 nM	Function Assay	6 h	inhibits mTORC1 activity by the dephosphorylation of S6 ribosomal protein	22401294
DND-1	0.25/0.5/1 μM	Growth Inhibition Assay	-	inhibits cell growth dose dependently	23482748
H116	0-1000 nM	Cell Viability Assay	24 h	inhibits the growth in a dose-dependent manner	23991179
HCT 116	-	Growth Inhibition Assay	-	IC50=0.41 μM	23542178
HCT 116	-	Growth Inhibition Assay	-	IC50=0.6 μM	22270257
HCT 15	-	Growth Inhibition Assay	-	IC50=0.3 μM	23542178
HCT15	0.5/2 μM	Function Assay	4 h	prevents S6K1 phosphorylation of ribosomal protein S6 at Ser240/244 and mTORC2 phosphorylation of Akt at Ser473	21876130
HCT-15	-	Growth Inhibition Assay	-	IC50=0.3 μM	22270257
Hct-8	0-1000 nM	Cell Viability Assay	24 h	inhibits the growth in a dose-dependent manner	23991179
HMEC	0-1000 nM	Cell Viability Assay	24/48 h	decreases cell viability in time and dose dependent manner	25035961
HT1376	-	Growth Inhibition Assay	-	IC50=1.88 ± 1.1 μM	24054871
HT29	1 μM	Function Assay	2 h	inhibits both mTORC1-mediated phosphorylation of S6K1 and mTORC2-mediated phosphorylation of Akt	25762619
HT29	1 μM	Function Assay	2 h	suppresses the basal or IGF-1-stimulated cell adhesion	25762619
HT29	0-1000 nM	Cell Viability Assay	24 h	inhibits the growth in a dose-dependent manner	23991179
HT29	1 μM	Function Assay	0-24 h	abolishes the S6S235/236 but partially reduces the 4E-BP1T36/45	23991179
HT-29	-	Growth Inhibition Assay	-	IC50=0.23 μM	23542178
HT-p21	50-1250 nM	Function Assay	24 h	inhibits phosphorylation of S6 kinase (target of mTORC1) and its downstream target phospho-S6	26177051
HUVEC	0-1000 nM	Cell Viability Assay	24/48 h	decreases cell viability in time and dose dependent manner	25035961
Jurkat	0.25/0.5/1 μM	Growth Inhibition Assay	-	inhibits cell growth dose dependently	23482748
Jurkat	100/200/400 nM	Function Assay	18 h	inhibits mTORC1-dependent S6 S235/236 phosphorylation	22566604
Jurkat	400nM	Growth Inhibition Assay	24/48 h	synergize with 17-AAG to suppress cell proliferation	22566604
KATO3	0-1000 nM	Cell Viability Assay	24/48 h	decreases cell viability in time and dose dependent manner	25035961
KOPT-K1	0.25/0.5/1 μM	Growth Inhibition Assay	-	inhibits cell growth dose dependently	23482748
LS174T	10/100/1000 nM	Function Assay	6 h	inhibits mTORC1 activity by the dephosphorylation of S6 ribosomal protein	22401294
LS-174T	-	Growth Inhibition Assay	-	IC50=0.84 μM	23542178
LS-513	-	Growth Inhibition Assay	-	IC50=3.9 μM	23542178
MCF-7	50/200/500 nM	Function Assay	30 min	dose-dependently (50–500 nM) suppresses phosphorylation of Akt	22476852
MCF-7	200 nM	Apoptosis Assay	36 h	induces apoptosis	22476852
MDA-MB-231	50/200/500 nM	Function Assay	30 min	dose-dependently (50–500 nM) suppresses phosphorylation of Akt	22476852
MDA-MB-231	200 nM	Apoptosis Assay	36 h	induces apoptosis	22476852
MG63	50-1000 nM	Function Assay	0.5 h	dose dependently (50–1000 nM) inhibits phosphorylation of Akt	24840134
MG63	100 nM	Apoptosis Assay	36 h	promotes apoptosis	24840134
MKN28	0-1000 nM	Cell Viability Assay	24/48 h	decreases cell viability in time and dose dependent manner	25035961
MKN45	0-1000 nM	Cell Viability Assay	24/48 h	decreases cell viability in time and dose dependent manner	25035961
MM1.S	100-1000 nM	Function Assay	30 min	activates ERK	22556409
MM1.S	0.5 μM	Function Assay	30 min	induces activation of RAF and phosphorylation of MEK	22556409
N87	0-1000 nM	Cell Viability Assay	24/48 h	decreases cell viability in time and dose dependent manner	25035961
NIH 3T3	2 μM	Function Assay	18 h	inhibits mTORC2 phosphorylation of Akt on Ser473 and mTORC1 phosphorylation of 4E-BP1 on Thr37/46	21876130
OCI-AML3	2.5 μM	Apoptosis Assay	72 h	induces apoptosis	22826565
p210 BCR-Abl	100/200/400 nM	Function Assay	18 h	inhibits mTORC1-dependent S6 S235/236 phosphorylation	22566604
p210 BCR-Abl	400nM	Growth Inhibition Assay	24/48 h	synergize with 17-AAG to suppress cell proliferation	22566604
PC12	40 nM	Function Assay	-	induces lysosomal biogenesis and alleviated α-SYN accumulation	26001614
Rh30	1 μM	Function Assay	2 h	inhibits both mTORC1-mediated phosphorylation of S6K1 and mTORC2-mediated phosphorylation of Akt	25762619
Rh30	1 μM	Function Assay	2 h	suppresses the basal or IGF-1-stimulated cell adhesion	25762619
Saos-2	50-1000 nM	Function Assay	0.5 h	dose dependently (50–1000 nM) inhibits phosphorylation of Akt	24840134
Saos-2	100 nM	Function Assay	0.5 h	prevents osteosarcoma cell migration	24840134
Saos-2	100 nM	Apoptosis Assay	36 h	promotes apoptosis	24840134
SGC7901	0-1000 nM	Cell Viability Assay	24/48 h	decreases cell viability in time and dose dependent manner	25035961
SK-CO-1	-	Growth Inhibition Assay	-	IC50=4 μM	23542178
SK-CO-1	-	Growth Inhibition Assay	-	IC50=2.1 μM	22270257
SW1116	-	Growth Inhibition Assay	-	IC50=0.84 μM	23542178
SW48	-	Growth Inhibition Assay	-	IC50=0.09 μM	23542178
SW-48	-	Growth Inhibition Assay	-	IC50=0.1 μM	22270257
SW480	-	Growth Inhibition Assay	-	IC50=4.6 μM	23542178
SW480	10/100/1000 nM	Function Assay	6 h	inhibits mTORC1 activity by the dephosphorylation of S6 ribosomal protein	22401294
SW620	-	Growth Inhibition Assay	-	IC50=7.8 μM	23542178
SW620	-	Growth Inhibition Assay	-	IC50=11 μM	22270257
SW620	0.5/2 μM	Function Assay	4 h	blocks all three mTOR outputs	21876130
SW620-R	-	Growth Inhibition Assay	-	IC50=1.3 μM	22270257
Sw948	0-1000 nM	Cell Viability Assay	24 h	inhibits the growth in a dose-dependent manner	23991179
Sw948	1 μM	Function Assay	0-24 h	abolishes the S6S235/236 but partially reduces the 4E-BP1T36/45	23991179
T24	-	Growth Inhibition Assay	-	IC50=1.37 ± 0.4 μM	24054871
T47D	50/200/500 nM	Function Assay	30 min	dose-dependently (50–500 nM) suppresses phosphorylation of Akt	22476852
THP-1	0.25/0.5/1 μM	Growth Inhibition Assay	-	inhibits cell growth dose dependently	23482748
TMD7	0.25/0.5/1 μM	Growth Inhibition Assay	-	inhibits cell growth dose dependently	23482748
TMD8	0.25/0.5/1 μM	Growth Inhibition Assay	-	inhibits cell growth dose dependently	23482748
U2OS	50-1000 nM	Function Assay	0.5 h	dose dependently (50–1000 nM) inhibits phosphorylation of Akt	24840134
U2OS	100 nM	Apoptosis Assay	36 h	promotes apoptosis	24840134
U87	25 nM	Growth Inhibition Assay	24 h	increases DUSP10 knocked-down induced cell inhibition	25568665
U87vIII	0.04-2.5 μM	Function Assay	24 h	inhibits mTORC1 and mTORC2 activities	26134617
U87vIII	2.5/5 μM	Function Assay	12 h	inhibits gap closing in a dose-dependent manner	26134617
UM-UC-3	-	Growth Inhibition Assay	-	IC50=0.63 ±0.1 μM	24054871

靶点	Description	IC50
Bromodomain 4		Kd:1.7μM
mTOR		IC50:8nM
p110δ		IC50:100nM

Torkinib Catalog No. CSN12732

靶点选择性

请登录您的专属账户

确认信息