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Orantinib {[allProObj[0].p_purity_real_show]}

货号:A670041 同义名: SU6668; TSU-68

Orantinib是一种多靶受体酪氨酸激酶抑制剂,IC50值分别为2.1 μM(VEGF-R1)、8 nM(PDGF-Rβ)和1.2 μM(FGF-R1)。

Orantinib 化学结构 CAS号:252916-29-3
Orantinib 化学结构
CAS号:252916-29-3
Orantinib 3D分子结构
CAS号:252916-29-3
Orantinib 化学结构 CAS号:252916-29-3
Orantinib 3D分子结构 CAS号:252916-29-3
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Orantinib 纯度/质量文件 产品仅供科研

货号:A670041 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 FGFR FGFR1 FGFR2 FGFR3 FGFR4 其他靶点 纯度
Tyrphostin AG1296 +

FGFR (Swiss 3T3), IC50: 12.3 μM

PDGFR 99%+
Pazopanib +

FGFR, IC50: 140 nM

99%
Erdafitinib RET 99%+
Gambogenic acid 98+%
Sulfatinib +++

FGFR1, IC50: 15 nM

99+%
Nintedanib esylate +

FGFR1, IC50: 69 nM

++

FGFR2, IC50: 37 nM

+

FGFR3, IC50: 108 nM

98%
Zoligratinib +++

FGFR1, IC50: 9.3 nM

+++

FGFR2, IC50: 7.6 nM

++

FGFR3, IC50: 22 nM

+

FGFR4, IC50: 290 nM

99%+
MK-2461 +

FGFR1, IC50: 65 nM

++

FGFR2, IC50: 39 nM

++

FGFR3, IC50: 50 nM

98%+
SU 5402 ++

FGFR1, IC50: 30 nM

98%
Brivanib +

FGFR1, IC50: 148 nM

99%+
Lucitanib ++

FGFR1, IC50: 17.5 nM

+

FGFR2, IC50: 82.5 nM

99%+
Ponatinib ++++

FGFR1, IC50: 2.2 nM

98%
PD-166866 +

FGFR1, IC50: 52.4 nM

99%
Narazaciclib ++

FGFR1, IC50: 26 nM

RET 99%+
Lactate +++

FGFR1, IC50: 8 nM

+++

FGFR3, IC50: 9 nM

c-Kit,FLT3 85%
Lenvatinib mesylate ++

FGFR1, IC50: 46 nM

c-RET 99%
LY2874455 ++++

FGFR1, IC50: 2.8 nM

++++

FGFR2, IC50: 2.6 nM

+++

FGFR3, IC50: 6.4 nM

+++

FGFR4, IC50: 6 nM

99%+
FIIN-2 +++

FGFR1, IC50: 3.09 nM

+++

FGFR2, IC50: 4.3 nM

++

FGFR3, IC50: 27 nM

++

FGFR4, IC50: 45.3 nM

99%
FIIN-3 +++

FGFR1, IC50: 13.1 nM

++

FGFR2, IC50: 21 nM

++

FGFR3, IC50: 31.4 nM

++

FGFR4, IC50: 35.3 nM

98%
Infigratinib ++++

FGFR1, IC50: 0.9 nM

++++

FGFR2, IC50: 1.4 nM

++++

FGFR3 (K650E), IC50: 4.9 nM

FGFR3, IC50: 1.0 nM

+

FGFR4, IC50: 60 nM

99%+
Danusertib ++

FGFR1, IC50: 47 nM

RET 99%+
R1530 ++

FGFR1, IC50: 28 nM

98%
ENMD-2076 +

FGFR1, IC50: 92.7 nM

+

FGFR2, IC50: 70.8 nM

RET,FLT3 98%
Dovitinib +++

FGFR1, IC50: 8 nM

+++

FGFR3, IC50: 9 nM

c-Kit,FLT3 99%+
Sorafenib +

FGFR1, IC50: 580 nM

99%
SSR128129E +

FGFR1, IC50: 1.9 μM

99%+
AZD-4547 ++++

FGFR1, IC50: 0.2 nM

++++

FGFR2, IC50: 2.5 nM

++++

FGFR3, IC50: 1.8 nM

98%
Lenvatinib ++

FGFR1, IC50: 46 nM

RET 98%
PD173074 ++

FGFR1, IC50: ~25 nM

99%+
S49076 ++

FGFR1, IC50: 18 nM

+++

FGFR2, IC50: 17 nM

+++

FGFR3, IC50: 15 nM

98%
Futibatinib ++++

FGFR1, IC50: 1.8 nM

++++

FGFR2, IC50: 1.4 nM

++++

FGFR3, IC50: 1.6 nM

+++

FGFR4, IC50: 3.7 nM

99%+
Ferulic Acid +

FGFR1, IC50: 3.78 μM

+

FGFR2, IC50: 12.5 μM

98%
Nintedanib +

FGFR1, IC50: 69 nM

++

FGFR2, IC50: 37 nM

+

FGFR3, IC50: 108 nM

+

FGFR4, IC50: 610 nM

99+%
ASP5878 ++++

FGFR1, IC50: 0.47 nM

++++

FGFR2, IC50: 0.6 nM

++++

FGFR3, IC50: 0.74 nM

+++

FGFR4, IC50: 3.5 nM

99%
PRN1371 ++++

FGFR1, IC50: 0.6 nM

++++

FGFR2, IC50: 1.3 nM

+++

FGFR3, IC50: 4.1 nM

++

FGFR4, IC50: 19.3 nM

99%
Derazantinib +++

FGFR1, IC50: 4.5 nM

++++

FGFR2, IC50: 1.8 nM

+++

FGFR3, IC50: 4.5 nM

++

FGFR4, IC50: 34 nM

RET 99%+
ODM-203 +++

FGFR1, IC50: 11 nM

+++

FGFR2, IC50: 16 nM

+++

FGFR3, IC50: 6 nM

++

FGFR4, IC50: 35 nM

99%+
Pemigatinib ++++

FGFR1, IC50: 0.4 nM

++++

FGFR2, IC50: 0.5 nM

++++

FGFR3, IC50: 1.2 nM

++

FGFR4, IC50: 30 nM

99%+
SKLB 610 PDGFR 99%+
Alofanib 99%+
Lirafugratinib 99%
Masitinib mesylate FAK 99%+
BLU9931 +

FGFR3, IC50: 150 nM

+++

FGFR4, IC50: 3 nM

99%+
BO-264 99%+
Fisogatinib +++

FGFR4, IC50: 5 nM

99%+
H3B-6527 ++++

FGFR4, IC50: <1.2 nM

99%+
Roblitinib ++++

FGFR4, IC50: 1.9 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, IC50: 3 nM

VEGFR2/Flk1, IC50: 3 nM

+++

VEGFR3, IC50: 6 nM

RET,PDGFR 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

c-Kit,PDGFR,FGFR 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

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

+++

hVEGFR2, IC50: 9 nM

mVEGF2, IC50: 165 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, IC50: 90 nM

VEGFR2/Flk1, 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。

Orantinib 生物活性

靶点
  • PDGFRβ

    PDGFRβ, Ki:8 nM

描述 TSU-68 is a multiple receptor tyrosine kinase inhibitor with IC50 of 2.1 μM, 8 nM and 1.2 μM for VEGF-R1, PDGF-Rβ and FGF-R1, respectively and has greatest potency against PDGFR autophosphorylation.

Orantinib 细胞实验

Cell Line
Concentration Treated Time Description References
Human Umbilical Vein Endothelial Cells (HUVECs) 10 ng/ml 3 days To investigate the effect of SU6668 on bFGF-induced HUVEC proliferation, results showed that SU6668 significantly inhibited the mitogenic effects of both bFGF and VEGF. Am J Pathol. 2002 Jun;160(6):2219-30.

Orantinib 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice RIP1Tag2 transgenic mice Oral 200 mg/kg Once daily, from 5 to 10.5 weeks of age (prevention trial), from 10 to 13.5 weeks of age (intervention trial), and from 12 to 16 weeks of age (regression trial) SU6668 was less effective in the prevention trial, but was much better in the regression trial, producing a condition of 'stable disease', reducing tumor burden and disrupting tumor vascularity. J Clin Invest. 2003 May;111(9):1287-95

Orantinib 参考文献

[1]Smolich BD, Yuen HA, et al. The antiangiogenic protein kinase inhibitors SU5416 and SU6668 inhibit the SCF receptor (c-kit) in a human myeloid leukemia cell line and in acute myeloid leukemia blasts. Blood. 2001 Mar 1;97(5):1413-21.

[2]Laird AD, Vajkoczy P, et al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60.

Orantinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.22mL

0.64mL

0.32mL

16.11mL

3.22mL

1.61mL

32.22mL

6.44mL

3.22mL

Orantinib 技术信息

CAS号252916-29-3
分子式C18H18N2O3
分子量 310.35
SMILES Code O=C(O)CCC1=C(C)NC(/C=C2C(NC3=C/2C=CC=C3)=O)=C1C
MDL No. MFCD09743433
别名 SU6668; TSU-68; NSC 702827
运输蓝冰
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

DMSO: 105 mg/mL(338.33 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

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
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