SP-96 is a highly selective and non-ATP-competitive Aurora A/B inhibitor with IC50 values of 0.316nM 18.975 nM for Aurora A and Aurora B, respectively.
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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 |
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CCT 137690 |
++
Aurora A, IC50: 15 nM |
++
Aurora B, IC50: 25 nM |
++
Aurora C, IC50: 19 nM |
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MK-5108 |
++++
Aurora A, IC50: 0.064 nM |
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KW-2449 |
+
Aurora A, IC50: 48 nM |
FLT3 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Tozasertib |
++++
Aurora A, Ki app: 0.6 nM |
++
Aurora B, Ki app: 18 nM |
+++
Aurora C, Ki app: 4.6 nM |
FLT3,Bcr-Abl | {[allProObj[0].p_purity_real_show]} | ||||||||||||||
AT9283 |
++++
Aurora A, IC50: ~3.0 nM |
++++
Aurora B, IC50: ~3.0 nM |
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MLN8054 |
+++
Aurora A, IC50: 4 nM |
+
Aurora B, IC50: 172 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
ZM-447439 |
+
Aurora A, IC50: 110 nM |
+
Aurora B, IC50: 130 nM |
Src | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
TCS7010 |
++++
Aurora A, IC50: 3.4 nM |
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TAK-901 |
++
Aurora A-TPX2, IC50: 21 nM |
++
Aurora B-INCENP, IC50: 15 nM |
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Danusertib |
+++
Aurora A, IC50: 13 nM |
+
Aurora B, IC50: 79 nM |
+
Aurora C, IC50: 61 nM |
RET | {[allProObj[0].p_purity_real_show]} | ||||||||||||||
MK-8745 |
++++
Aurora A, IC50: 0.6 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
PHA-680632 |
++
Aurora A, IC50: 27 nM |
+
Aurora B, IC50: 135 nM |
+
Aurora C, IC50: 120 nM |
FLT3 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||
AMG 900 |
+++
Aurora A, IC50: 5 nM |
+++
Aurora B, IC50: 4 nM |
++++
Aurora C, IC50: 1 nM |
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Alisertib |
++++
Aurora A, IC50: 1.2 nM |
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ENMD-2076 |
+++
Aurora A, IC50: 14 nM |
+
Aurora B, IC50: 350 nM |
FLT3,RET | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
JNJ-7706621 |
+++
Aurora A, IC50: 11 nM |
++
Aurora B, IC50: 15 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
CYC-116 |
+++
Aurora A, Ki: 8 nM |
+++
Aurora B, Ki: 9 nM |
FLT3 | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
Reversine |
+++
Aurora A, IC50: 12 nM |
+++
Aurora B, IC50: 13 nM |
++
Aurora C, IC50: 20 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
CCT129202 |
++
Aurora A, IC50: 42 nM |
+
Aurora B, IC50: 198 nM |
+
Aurora C, IC50: 227 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
SNS-314 mesylate |
+++
Aurora A, IC50: 9 nM |
++
Aurora B, IC50: 31 nM |
++++
Aurora C, IC50: 3 nM |
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Barasertib-HQPA |
++++
Aurora B, IC50: 0.37 nM |
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Hesperadin |
+
Aurora B (human), IC50: 250 nM |
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GSK-1070916 |
++++
Aurora B-INCENP, IC50: 3.5 nM |
+++
Aurora C-INCENP, IC50: 6.5 nM |
SIK,Tie-2 | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
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 | SP-96 is a potent, selective, and non-ATP-competitive inhibitor of Aurora B (IC50=0.316 nM), with >2000 fold selectivity against FLT3 and KIT. It demonstrates selective growth inhibition in NCI60 screening, including MDA-MD-468 (GI50=107 nM). SP-96 is a valuable tool for researching triple negative breast cancer (TNBC)[1]. |
体外研究 | SP-96 is a potent, selective, and non-ATP-competitive inhibitor of Aurora B (IC50=0.316 nM), exhibiting over 2000-fold selectivity against FLT3 (IC50=1475.6 nM) and KIT (IC50=1307.6 nM)[1]. SP-96 (0-1 µM; 24 hours) exhibits selectivity rather than promiscuity towards specific cell lines. It inhibits the growth of MDA-MB-468, CCRF-CEM, COLO 205, and A498 cells with GI50 values of 107 nM, 47.4 nM, 50.3 nM, and 53.2 nM, respectively[1]. SP-96 (63.2 nM) suppresses Aurora B activity in H460 cells, leading to increased DNA content and enlarged cell volume with enlarged nuclei[1]. SP-96 (0-2 µM) suppresses Aurora B enzymatic activity with an IC50 of 0.316 nM and Aurora A with an observed IC50 value of 18.975 nM. It demonstrates over 2000-fold selectivity against FLT3 (IC50=1475.6 nM) and KIT (IC50=1307.6 nM). Additionally, it inhibits other receptor tyrosine kinases (RTKs) such as EGFR, RET, and HER2, with IC50 values ≥2 µM[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.21mL 0.44mL 0.22mL |
11.03mL 2.21mL 1.10mL |
22.05mL 4.41mL 2.21mL |
CAS号 | 2682114-54-9 |
分子式 | C25H20FN7O |
分子量 | 453.471 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(231.55 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 |