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PP121 {[allProObj[0].p_purity_real_show]}

货号:A986976

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 化学结构 CAS号:1092788-83-4
PP121 化学结构
CAS号:1092788-83-4
PP121 3D分子结构
CAS号:1092788-83-4
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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PP121 纯度/质量文件 产品仅供科研

货号:A986976 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 mTOR mTORC1 mTORC2 其他靶点 纯度
AZD-8055 ++++

mTOR (truncated), IC50: 0.13 nM

mTOR (full length), IC50: 0.8 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

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

98%
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

mTOR,VEGFR 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 98+%
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 98%
Dovitinib +++

PDGFRβ, IC50: 27 nM

c-Kit,FLT3 99%+
Sorafenib ++

mPDGFRβ, IC50: 57 nM

PDGFRβ, 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 98%
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

c-Kit,FGFR,PDGFR 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/KDR, IC50: 37 nM

VEGFR2/Flk1, IC50: 270 nM

+

VEGFR3/FLT4, IC50: 660 nM

c-Kit,c-Fms 99%+
Axitinib ++++

VEGFR1/FLT1, IC50: 0.1 nM

++++

VEGFR2/KDR, IC50: 0.2 nM

VEGFR2/Flk1, IC50: 0.18 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

c-Kit,BTK 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

98%
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

98%
Cabozantinib S-malate ++++

VEGFR2/KDR, IC50: 0.035 nM

99+%
Ki8751 ++++

VEGFR2, IC50: 0.9 nM

c-Kit 98+%
SU 5402 ++

VEGFR2, IC50: 20 nM

98%
Rivoceranib 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 98%
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 98%
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 参考文献

[1]Peng Y, Zhou Y, et al. The anti-esophageal cancer cell activity by a novel tyrosine/phosphoinositide kinase inhibitor PP121. Biochem Biophys Res Commun. 2015 Sep 11;465(1):137-44.

[2]Apsel B, Blair JA, et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.

PP121 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.13mL

0.63mL

0.31mL

15.66mL

3.13mL

1.57mL

31.31mL

6.26mL

3.13mL

PP121 技术信息

CAS号1092788-83-4
分子式C17H17N7
分子量 319.364
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 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 18 mg/mL(56.36 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
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