CTX-0294885是一种双苯胺嘧啶类化合物,在体外对广泛的激酶具有抑制活性,进一步开发为Sepharose支持的激酶捕获试剂。CTX-0294885 在初步筛选中抑制了FAK、FLT3、JAK2、JAK3、Src、Aurora激酶A和VEGF受体3,IC50分别为4、1、3、28、2、18和3 nM。


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| 产品名称 | Aurora A ↓ ↑ | Aurora B ↓ ↑ | Aurora C ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| BI-847325 |
++
Aurora A (Human), IC50: 25 nM |
++++
Aurora B (Xenopus laevis), IC50: 3 nM |
++
Aurora C (Human), IC50: 15 nM |
99%+ | |||||||||||||||
| CCT 137690 |
++
Aurora A, IC50: 15 nM |
++
Aurora B, IC50: 25 nM |
++
Aurora C, IC50: 19 nM |
99%+ | |||||||||||||||
| MK-5108 |
++++
Aurora A, IC50: 0.064 nM |
99%+ | |||||||||||||||||
| KW-2449 |
+
Aurora A, IC50: 48 nM |
FLT3 | 99%+ | ||||||||||||||||
| Tozasertib |
++++
Aurora A, Ki app: 0.6 nM |
++
Aurora B, Ki app: 18 nM |
+++
Aurora C, Ki app: 4.6 nM |
FLT3,Bcr-Abl | 99%+ | ||||||||||||||
| AT9283 |
++++
Aurora A, IC50: ~3.0 nM |
++++
Aurora B, IC50: ~3.0 nM |
99%+ | ||||||||||||||||
| MLN8054 |
+++
Aurora A, IC50: 4 nM |
+
Aurora B, IC50: 172 nM |
99%+ | ||||||||||||||||
| ZM-447439 |
+
Aurora A, IC50: 110 nM |
+
Aurora B, IC50: 130 nM |
Src | 99%+ | |||||||||||||||
| TCS7010 |
++++
Aurora A, IC50: 3.4 nM |
99%+ | |||||||||||||||||
| TAK-901 |
++
Aurora A-TPX2, IC50: 21 nM |
++
Aurora B-INCENP, IC50: 15 nM |
99%+ | ||||||||||||||||
| Danusertib |
+++
Aurora A, IC50: 13 nM |
+
Aurora B, IC50: 79 nM |
+
Aurora C, IC50: 61 nM |
RET | 99%+ | ||||||||||||||
| MK-8745 |
++++
Aurora A, IC50: 0.6 nM |
99+% | |||||||||||||||||
| PHA-680632 |
++
Aurora A, IC50: 27 nM |
+
Aurora B, IC50: 135 nM |
+
Aurora C, IC50: 120 nM |
FLT3 | 99%+ | ||||||||||||||
| AMG 900 |
+++
Aurora A, IC50: 5 nM |
+++
Aurora B, IC50: 4 nM |
++++
Aurora C, IC50: 1 nM |
99%+ | |||||||||||||||
| Alisertib |
++++
Aurora A, IC50: 1.2 nM |
99%+ | |||||||||||||||||
| ENMD-2076 |
+++
Aurora A, IC50: 14 nM |
+
Aurora B, IC50: 350 nM |
FLT3,RET | 98% | |||||||||||||||
| JNJ-7706621 |
+++
Aurora A, IC50: 11 nM |
++
Aurora B, IC50: 15 nM |
99%+ | ||||||||||||||||
| CYC-116 |
+++
Aurora A, Ki: 8 nM |
+++
Aurora B, Ki: 9 nM |
FLT3 | 99%+ | |||||||||||||||
| Reversine |
+++
Aurora A, IC50: 12 nM |
+++
Aurora B, IC50: 13 nM |
++
Aurora C, IC50: 20 nM |
98% | |||||||||||||||
| CCT129202 |
++
Aurora A, IC50: 42 nM |
+
Aurora B, IC50: 198 nM |
+
Aurora C, IC50: 227 nM |
98% | |||||||||||||||
| SNS-314 mesylate |
+++
Aurora A, IC50: 9 nM |
++
Aurora B, IC50: 31 nM |
++++
Aurora C, IC50: 3 nM |
99%+ | |||||||||||||||
| Barasertib-HQPA |
++++
Aurora B, IC50: 0.37 nM |
99%+ | |||||||||||||||||
| Hesperadin |
+
Aurora B (human), IC50: 250 nM |
98% | |||||||||||||||||
| GSK-1070916 |
++++
Aurora B-INCENP, IC50: 3.5 nM |
+++
Aurora C-INCENP, IC50: 6.5 nM |
SIK,Tie-2 | 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 (D835Y), IC50: 0.4 nM FLT3, 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 | FAK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Defactinib | ✔ | 99%+ | |||||||||||||||||
| NVP-TAE 226 |
++
FAK, IC50: 5.5 nM PYK2, IC50: 3.5 nM |
IGF-1R,Insulin Receptor | 98+% | ||||||||||||||||
| PF-573228 |
+
FAK, IC50: 4 nM |
98% | |||||||||||||||||
| Solanesol | ✔ | 90% +(HPLC) | |||||||||||||||||
| PF-431396 |
++
FAK, IC50: 2 nM PYK2, IC50: 11 nM |
99%+ | |||||||||||||||||
| PND-1186 |
++++
FAK, IC50: 1.5 nM |
99%+ | |||||||||||||||||
| PF-562271 |
++++
FAK, IC50: 1.5 nM PYK2, IC50: 13 nM |
99%+ | |||||||||||||||||
| GSK2256098 |
++++
FAK, Ki: 0.4 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 | JAK1 ↓ ↑ | JAK2 ↓ ↑ | JAK3 ↓ ↑ | Tyk2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Decernotinib |
+++
JAK1, Ki: 11 nM JAK1, IC50: 11 nM |
+++
JAK2, Ki: 13 nM |
++++
JAK3, Ki: 2.5 nM |
+++
TYK2, Ki: 13 nM |
99%+ | ||||||||||||||
| ZM39923 HCl |
+
JAK1, pIC50: 4.4 |
+
JAK3, pIC50: 7.1 |
EGFR | 97% | |||||||||||||||
| Cerdulatinib |
+++
JAK1, IC50: 12 nM |
+++
JAK2, IC50: 6 nM |
+++
JAK3, IC50: 8 nM |
++++
TYK2, IC50: 0.5 nM |
99%+ | ||||||||||||||
| Momelotinib |
+++
JAK1, IC50: 11 nM |
++
JAK2, IC50: 18 nM |
+
JAK3, IC50: 155 nM |
99%+ | |||||||||||||||
| XL019 |
+
JAK1, IC50: 134.3 nM |
++++
JAK2, IC50: 2.2 nM |
+
JAK3, IC50: 214.2 nM |
FLT3 | 99%+ | ||||||||||||||
| Ruxolitinib |
+++
JAK1, IC50: 3.3 nM |
++++
JAK2, IC50: 2.8 nM |
98% | ||||||||||||||||
| Tofacitinib |
+
JAK1, IC50: 112 nM |
++
JAK2, IC50: 20 nM |
++++
JAK3, IC50: 1 nM |
98% | |||||||||||||||
| Ruxolitinib (S enantiomer) |
+++
JAK1, IC50: 3.3 nM |
++++
JAK2, IC50: 2.8 nM |
++
TYK2, IC50: 19 nM |
98% | |||||||||||||||
| Filgotinib |
+++
JAK1, IC50: 10 nM |
++
JAK2, IC50: 28 nM |
+
JAK3, IC50: 810 nM |
+
TYK2, IC50: 116 nM |
99% | ||||||||||||||
| Baricitinib |
+++
JAK1, IC50: 5.9 nM |
+++
JAK2, IC50: 5.7 nM |
++
TYK2, IC50: 53 nM |
99% | |||||||||||||||
| Gandotinib |
++
JAK1, IC50: 19.8 nM |
++++
JAK2, IC50: 0.288 nM JAK2 (V617F), Ki: 0.245 nM |
++
JAK3, IC50: 48.0 nM |
++
TYK2, IC50: 44 nM |
FLT3 | 99%+ | |||||||||||||
| Oclacitinib maleate |
+++
JAK1, IC50: 10nM |
++
JAK2, IC50: 18nM |
+
JAK3, IC50: 99nM |
+
TYK2, IC50: 84nM |
98+% | ||||||||||||||
| NVP-BSK805 2HCl |
++
JAK1, IC50: 31.63 nM |
++++
JAK2, IC50: ~0.5 nM |
++
JAK3, IC50: 18.68 nM |
+++
TYK2, IC50: 10.76 nM |
95% | ||||||||||||||
| Peficitinib | ✔ | 98% | |||||||||||||||||
| Go6976 | ✔ | FLT3 | 99%+ | ||||||||||||||||
| AZD-1480 |
++++
JAK2, IC50: 0.26 nM |
99%+ | |||||||||||||||||
| Fedratinib |
+++
JAK2 (V617F), IC50: 3 nM JAK2, IC50: 3 nM |
FLT3,RET | 99%+ | ||||||||||||||||
| WP1066 |
+
JAK2, IC50: 2.3 μM |
98% | |||||||||||||||||
| Curcumol | ✔ | 98% | |||||||||||||||||
| AZ960 |
++++
JAK2, IC50: <3 nM JAK2, Ki: 0.45 nM |
97% | |||||||||||||||||
| GLPG0634 analog | ✔ | 99%+ | |||||||||||||||||
| CEP-33779 |
++++
JAK2, IC50: 1.8 nM |
99%+ | |||||||||||||||||
| FLLL32 |
+
JAK2, IC50: <5 μM |
99%+ | |||||||||||||||||
| WHI-P154 |
+
JAK3, IC50: 1.8 μM |
EGFR,VEGFR,Src | 98% | ||||||||||||||||
| BMS-911543 |
++++
JAK2, IC50: 1.1 nM |
+
JAK3, IC50: 75 nM |
++
TYK2, IC50: 66 nM |
95% | |||||||||||||||
| TG101209 |
+++
JAK2, IC50: 6 nM |
+
JAK3, IC50: 169 nM |
RET,FLT3 | 99%+ | |||||||||||||||
| AT9283 |
++++
JAK2, IC50: 1.2 nM |
++++
JAK3, IC50: 1.1 nM |
99%+ | ||||||||||||||||
| Pacritinib |
++
JAK2 (V617F), IC50: 19 nM JAK2, IC50: 23 nM |
+
JAK3, IC50: 520 nM |
++
TYK2, IC50: 50 nM |
FLT3 | 97% | ||||||||||||||
| Tofacitinib citrate |
++
JAK2, IC50: 20 nM |
++++
JAK3, IC50: 1 nM |
99% | ||||||||||||||||
| FM-381 |
++++
JAK3, IC50: 127 pM |
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 | 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 |
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,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 |
FLT3,c-Kit | 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-Fms/CSF1R,c-Kit | 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 |
FLT3,c-Kit | 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 |
+++
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/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 |
FLT3,RET | 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。 | |||||||||||||||||||
| 描述 | CTX-0294885 is a broad-spectrum kinase inhibitor capable of targeting 235 kinases in MDA-MB-231 cells, including all members of the AKT family, marking its utility in dissecting kinome signaling pathways for the study of diseases such as inflammation, diabetes, and cancer. |
| 体外研究 | CTX-0294885 is a valuable tool in kinome profiling experiments, capturing a wide array of kinases, and its unique ability to isolate all AKT family members highlights its potential in uncovering new aspects of kinase-related research previously unexplored with other kinase capture agents. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.28mL 0.46mL 0.23mL |
11.42mL 2.28mL 1.14mL |
22.83mL 4.57mL 2.28mL |
|
| CAS号 | 1439934-41-4 |
| 分子式 | C22H24ClN7O |
| 分子量 | 437.93 |
| SMILES Code | O=C(NC)C1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCNCC4)C=C3)=NC=C2Cl |
| MDL No. | MFCD28137930 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | FCLOIQHNUARDSR-UHFFFAOYSA-N |
| Pubchem ID | 71558939 |
| 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: 105 mg/mL(239.77 mM),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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