XL228是一种多靶点蛋白激酶抑制剂,对Bcr-Abl、Aurora A、IGF-1R、Src和Lyn的IC50分别为5 nM、3.1 nM、1.6 nM、6.1 nM和2 nM。


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| 产品名称 | ALK1 ↓ ↑ | ALK2 ↓ ↑ | ALK3 ↓ ↑ | ALK4 ↓ ↑ | ALK6 ↓ ↑ | Smad3 ↓ ↑ | TGF-β ↓ ↑ | TGFβRI/ALK5 ↓ ↑ | TGFβRII ↓ ↑ | 其他靶点 | 纯度 | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| LDN193189 |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99%+ | ||||||||||||||
| LDN-212854 |
++++
ALK1, IC50: 2.4 nM |
++++
ALK2, IC50: 1.3 nM |
+
ALK3, IC50: 85.8 nM |
+
ALK4, IC50: 2133 nM |
+
ALK5, IC50: 9276 nM |
99%+ | |||||||||||||
| ML347 |
++
ALK1, IC50: 46 nM |
++
ALK2, IC50: 32 nM |
98% | ||||||||||||||||
| K02288 |
++++
ALK1, IC50: 1.8 nM |
++++
ALK2, IC50: 1.1 nM |
++
ALK3, IC50: 34.4 nM |
+++
ALK6, IC50: 6.4 nM |
99%+ | ||||||||||||||
| LDN-193189 2HCl |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99% | ||||||||||||||
| LDN-214117 |
++
ALK2, IC50: 24 nM |
98% | |||||||||||||||||
| DMH-1 |
+
ALK2, IC50: 107.9 nM |
99%+ | |||||||||||||||||
| SB-505124 |
+
ALK4, IC50: 129 nM |
++
ALK5, IC50: 47 nM |
99%+ | ||||||||||||||||
| Vactosertib |
+++
ALK4, IC50: 13 nM |
+++
ALK5, IC50: 11 nM |
99%+ | ||||||||||||||||
| Alantolactone | ✔ | 98% | |||||||||||||||||
| (E/Z)-SIS3 free base | ✔ | 97% | |||||||||||||||||
| Pirfenidone | ✔ | 98% | |||||||||||||||||
| Hesperetin | ✔ | 97% | |||||||||||||||||
| RepSox |
++++
TGFβR1(ALK5), IC50: 4 nM |
98% | |||||||||||||||||
| GW788388 |
+++
ALK5, IC50: 18 nM |
98% | |||||||||||||||||
| LY364947 |
++
TGFβRI, IC50: 59 nM |
+
TGFβRII, IC50: 0.4 μM |
98% | ||||||||||||||||
| SD-208 |
++
TGF-βRI (ALK5), IC50: 48 nM |
99% | |||||||||||||||||
| SB-525334 |
+++
TGFβR1(ALK5), IC50: 14.3 nM |
99%+ | |||||||||||||||||
| LY2109761 |
++
TβRI, Ki: 38 nM |
+
TβRII, Ki: 300 nM |
99%+ | ||||||||||||||||
| Galunisertib |
++
TβRI, IC50: 56 nM |
98% | |||||||||||||||||
| SB 431542 |
+
ALK5, IC50: 94 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 | IGF-1R ↓ ↑ | Insulin Receptor ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| BMS-536924 |
++
IGF-1R, IC50: 100 nM |
+++
Insulin Receptor, IC50: 73 nM |
MEK,FAK | 98% | |||||||||||||||
| GSK1904529A |
+++
IGF-1R, IC50: 27 nM |
+++
Insulin Receptor, IC50: 25 nM |
98+% | ||||||||||||||||
| Picropodophyllin |
++++
IGF-1R, IC50: 1 nM |
99%+ | |||||||||||||||||
| NVP-AEW541 |
++
IGF-1R, IC50: 0.15 μM |
++
Insulin Receptor, IC50: 0.14 μM |
FLT3 | 99%+ | |||||||||||||||
| NVP-ADW742 |
+
IGF-1R, IC50: 0.17 μM |
98% | |||||||||||||||||
| GSK1838705A |
+++
IGF-1R, IC50: 2 nM |
++++
Insulin Receptor, IC50: 1.6 nM |
ALK | 98% | |||||||||||||||
| BMS-754807 |
++++
IGF-1R, IC50: 1.8 nM |
++++
Insulin Receptor, IC50: 1.7 nM |
99%+ | ||||||||||||||||
| Linsitinib |
+++
IGF-1R, IC50: 35 nM |
++
Insulin Receptor, IC50: 75 nM |
99%+ | ||||||||||||||||
| AG1024 |
+
IGF-1R, IC50: 7 μM |
+
Insulin Receptor, IC50: 57 μM |
98% | ||||||||||||||||
| PQ401 |
+
IGF-1R, IC50: <1 μM |
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 | 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 | Abl ↓ ↑ | Bcr-Abl ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| NVP-BHG 712 |
+
c-Abl, IC50: 1.667 μM |
99%+ | |||||||||||||||||
| KW-2449 |
+++
Abl, IC50: 14 nM Abl (T315I), IC50: 4 nM |
FLT3 | 99%+ | ||||||||||||||||
| Ponatinib |
++++
Abl, IC50: 0.37 nM |
98% | |||||||||||||||||
| AT9283 | 99%+ | ||||||||||||||||||
| Imatinib Mesylate |
+
v-Abl, IC50: 600 nM |
c-Kit,PDGFR | 99% | ||||||||||||||||
| Danusertib |
++
Abl, IC50: 25 nM |
RET | 99%+ | ||||||||||||||||
| Rebastinib |
++++
u-Abl1 (T315I), IC50: 5 nM p-Abl1 (native), IC50: 0.75 nM |
FLT3,Tie-2 | 99%+ | ||||||||||||||||
| PP121 |
++
Abl, IC50: 18 nM |
VEGFR,PDGFR | 99%+ | ||||||||||||||||
| GNF-7 |
+++
M351T, IC50: 133 nM E255V, IC50: 122 nM |
99%+ | |||||||||||||||||
| Olverembatinib dimesylate |
++++
Abl, IC50: 0.34 nM Abl (G250E), IC50: 0.35 nM |
98% | |||||||||||||||||
| Dasatinib monohydrate |
++++
Abl , IC50: 0.6 nM |
Src | 98% | ||||||||||||||||
| Dasatinib |
++++
Abl, IC50: 0.6 nM |
Src | 98% | ||||||||||||||||
| Bafetinib |
+++
Abl, IC50: 5.8 nM |
98+% | |||||||||||||||||
| GNF-2 |
+
Bcr-Abl (SUP-B15 cell line), IC50: 268 nM Bcr-Abl (K562 cell line), IC50: 273 nM |
98%+ | |||||||||||||||||
| Degrasyn |
+
Bcr-Abl, IC50: 1.8 μM |
DUB/Deubiquitinase | 99+% | ||||||||||||||||
| GNF-5 |
++
Bcr-Abl, IC50: 220 nM |
99% | |||||||||||||||||
| Radotinib |
++
BCR-ABL1, IC50: 34 nM |
98+% | |||||||||||||||||
| PD173955 | Src | 99%+ | |||||||||||||||||
| Nilotinib |
++
Bcr-Abl, IC50: <30 nM |
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 | Fyn ↓ ↑ | Lck ↓ ↑ | Lyn ↓ ↑ | Src ↓ ↑ | Yes ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Saracatinib |
++
Fyn, IC50: 10 nM |
++++
LCK, IC50: <4 nM |
+++
Lyn, IC50: 5 nM |
++++
c-Src, IC50: 2.7 nM |
99%+ | ||||||||||||||
| SU6656 |
+
Fyn, IC50: 170 nM |
+
Lyn, IC50: 130 nM |
+
Src, IC50: 280 nM |
++
YES, IC50: 20 nM |
98% | ||||||||||||||
| PP1 |
+++
Fyn, IC50: 6 nM |
+++
LCK, IC50: 5 nM |
EGFR | 99%+ | |||||||||||||||
| PP2 |
+++
Fyn, IC50: 5 nM |
++++
LCK, IC50: 4 nM |
98% | ||||||||||||||||
| WH-4-023 |
++++
Lck, IC50: 2 nM |
+++
Src, IC50: 6 nM |
99%+ | ||||||||||||||||
| NVP-BHG 712 |
+
c-Src, IC50: 1.266 μM |
99%+ | |||||||||||||||||
| CCT196969 |
++
LCK, IC50: 0.02 μM |
+
Src, IC50: 0.03 μM |
98% | ||||||||||||||||
| MNS |
+
Src, IC50: 29.3 μM |
p97,Syk | 98% | ||||||||||||||||
| Tirbanibulin |
++
Src (HuH7), GI50: 13 nM Src (Hep 3B), GI50: 26 nM |
99%+ | |||||||||||||||||
| PP121 |
++
Src, IC50: 14 nM |
VEGFR,PDGFR | 99%+ | ||||||||||||||||
| Bosutinib |
++++
Src, IC50: 1.2 nM |
99% | |||||||||||||||||
| Dasatinib monohydrate |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
| Quercetin | ✔ | PKC,Sirtuin | 95% | ||||||||||||||||
| Dasatinib |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
| Repotrectinib |
+++
Src, IC50: 5.3 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。 | |||||||||||||||||||
| 描述 | XL228 is a protein kinase inhibitor targeting IGF1R, the Aurora kinases, FGFR1-3, ABL and SRC family kinases. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.29mL 0.46mL 0.23mL |
11.43mL 2.29mL 1.14mL |
22.86mL 4.57mL 2.29mL |
|
| CAS号 | 898280-07-4 |
| 分子式 | C22H31N9O |
| 分子量 | 437.54 |
| SMILES Code | CN1CCN(C2=CC(NC3=NNC(C4CC4)=C3)=NC(NCC5=CC(C(C)C)=NO5)=N2)CC1 |
| MDL No. | MFCD26793867 |
| 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 Keep in dark place, inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 85 mg/mL(194.27 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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