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| 产品名称 | c-Kit ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Tyrphostin AG1296 |
+
c-Kit (Swiss 3T3), IC50: 1.8 μM |
PDGFR | 99%+ | ||||||||||||||||
| Masitinib |
+
Kit, IC50: 200 nM |
99%+ | |||||||||||||||||
| Motesanib Diphosphate |
+++
Kit, IC50: 8 nM |
97% | |||||||||||||||||
| Ki8751 |
++
c-Kit, IC50: 40 nM |
99% | |||||||||||||||||
| Tivozanib |
++
c-Kit, IC50: 78 nM |
99%+ | |||||||||||||||||
| Pazopanib |
+
c-Kit, IC50: 140 nM |
99% | |||||||||||||||||
| Sitravatinib |
+++
Kit, IC50: 6 nM |
99%+ | |||||||||||||||||
| Pexidartinib |
+++
Kit, IC50: 10 nM |
99%+ | |||||||||||||||||
| Lactate |
++++
c-Kit, IC50: 2 nM |
FLT3 | 85% | ||||||||||||||||
| Amuvatinib |
+++
c-Kit (D816H), IC50: 10 nM |
99%+ | |||||||||||||||||
| Imatinib Mesylate |
+
c-Kit, IC50: 100 nM |
PDGFR | 99% | ||||||||||||||||
| AZD2932 |
+++
c-Kit, IC50: 9 nM |
99% | |||||||||||||||||
| Axitinib |
++++
Kit, IC50: 1.7 nM |
98% | |||||||||||||||||
| Dovitinib |
++++
c-Kit, IC50: 2 nM |
FLT3 | 99%+ | ||||||||||||||||
| Sunitinib | ✔ | FLT3 | 98% | ||||||||||||||||
| OSI-930 |
+
Kit, IC50: 80 nM |
99%+ | |||||||||||||||||
| Telatinib |
++++
c-Kit, IC50: 1 nM |
99%+ | |||||||||||||||||
| Dasatinib monohydrate |
++
c-Kit (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 nM |
Src | 98% | ||||||||||||||||
| Dasatinib |
++
c-Kit (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 nM |
Src | 98% | ||||||||||||||||
| 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 | FLT3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| R406 | ✔ | Syk | 98% | ||||||||||||||||
| Go6976 | ✔ | 99%+ | |||||||||||||||||
| Quizartinib |
+++
FLT3 (ITD), IC50: 1.1 nM FLT3 (WT), IC50: 4.2 nM |
98% | |||||||||||||||||
| Gilteritinib |
++++
FLT3, IC50: 0.29 nM |
99%+ | |||||||||||||||||
| Amuvatinib |
+
FLT3 (D835Y), IC50: 81 nM |
99%+ | |||||||||||||||||
| Pacritinib |
++
FLT3, IC50: 22 nM FLT3 (D835Y), IC50: 6 nM |
97% | |||||||||||||||||
| Dovitinib |
++++
FLT3, IC50: 1 nM |
c-Kit | 99%+ | ||||||||||||||||
| Denfivontinib |
++++
FLT3, IC50: 0.4 nM FLT3 (D835Y), IC50: 0.4 nM |
RET | 99%+ | ||||||||||||||||
| TAK-659 HCl |
++
FLT3, IC50: 4.6 nM |
Syk | 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。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | AZD2932 has a potent and balanced profile against PDGFβ, VEGFR-2, Flt-3 and c-Kit. It does not inhibit the various cytochrome P450 isoforms with the worst IC50 being against 2C9 (8.0 μM). AZD2932 has no activity against hERG (IC50=137 μM)[1]. |
| 体内研究 | The efficacy of AZD2932 in tumor growth inhibition was demonstrated through oral administration twice daily in xenograft models, achieving significant tumor growth reduction at both 50 and 12.5 mg/kg doses. This effect was consistent across xenografts with and without PDGFβ expressing tumor cells, suggesting the compound's broad anti-tumor activity is not solely dependent on PDGFβ inhibition. The inhibition of VEGFR2, as well as potential effects on pericytes and tumor-associated fibroblasts through PDGFR α and β inhibition, likely contribute to its efficacy. This broad-spectrum activity against key angiogenesis and tumor growth pathways suggests AZD2932 could have a significant therapeutic impact on various cancers[1]. |
| 体外研究 | AZD2932 has a potent and balanced profile against PDGFβ, VEGFR-2, Flt-3 and c-Kit. It does not inhibit the various cytochrome P450 isoforms with the worst IC50 being against 2C9 (8.0 μM). AZD2932 has no activity against hERG (IC50=137 μM)[1]. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.23mL 0.45mL 0.22mL |
11.17mL 2.23mL 1.12mL |
22.35mL 4.47mL 2.23mL |
|
| CAS号 | 883986-34-3 |
| 分子式 | C24H25N5O4 |
| 分子量 | 447.49 |
| SMILES Code | O=C(NC1=CN(C(C)C)N=C1)CC2=CC=C(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)C=C2 |
| MDL No. | MFCD25977021 |
| 别名 | |
| 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, 2-8°C |
| 溶解方案 |
DMSO: 9 mg/mL(20.11 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 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
|
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