您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Ilorasertib
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Ilorasertib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ilorasertib图片
CAS NO:1227939-82-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
ABT-348
产品介绍
Ilorasertib (ABT-348) 是一种有效的,具有口服活性和 ATP 竞争性的aurora抑制剂,对 aurora A, aurora B, aurora C 的IC50值分别为 116, 5, 1 nM。Ilorasertib 也是一种有效的VEGFPDGF抑制剂。Ilorasertib 具有用于急性髓系白血病 (AML) 和骨髓增生异常综合征 (MDS) 的研究潜力。
生物活性

Ilorasertib (ABT-348) is a potent, orally active and ATP-competitiveaurorainhibitor withIC50s of116, 5, 1 nM foraurora A,aurora B,aurora C, respectively. Ilorasertib also is a potentVEGF,PDGFinhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS)[1][2].

IC50& Target[1]

Aurora C

1 nM (IC50)

Aurora B

7 nM (IC50)

Aurora B (Y156H)

12 nM (IC50)

Aurora A

120 nM (IC50)

PDGFRα

11 nM (IC50)

PDGFRβ

13 nM (IC50)

VEGFR1

1 nM (IC50)

VEGFR2

2 nM (IC50)

VEGFR3

43 nM (IC50)

FLT3

1 nM (IC50)

CSF-1R

3 nM (IC50)

c-KIT

20 nM (IC50)

体外研究
(In Vitro)

Ilorasertib (0, 3, 10, 30 nM; 24 h) induces a concentration-dependent increase in the extent and number of H1299, H460 cells[2].
Ilorasertib (1-1000 nM) shows antiproliferative activity[2].

Cell Viability Assay[2]

Cell Line:H1299, H460 cells
Concentration:0, 3, 10, 30 nM
Incubation Time:24 h
Result:Induced a concentration-dependent increase in the extent and number of cells exhibiting polyploidy with EC50S of 5, 10 nM for H1299, H460 cells, respectively.

Cell Proliferation Assay[2]

Cell Line:MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells
Concentration:1-1000 nM
Incubation Time:
Result:Showed antiproliferative activity with IC50s of 0.3, 1, 103, 6, 6, 2, 2 nM for MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells, respectively.
体内研究
(In Vivo)

Ilorasertib (6.25, 12.5, 25 mg/kg; p.o.) shows anti-tumor activity in MV-4-11 tumor-bearing SCID mice with TGI of 80%, 86%, 94% at 6.25, 12.5, 25 mg/kg, respectively[1].
Ilorasertib (6.25, 12.5, 25 mg/kg; p.o.) shows anti-tumor activity in SKM-1 tumor-bearing SCID mice with TGI of 38%, 59%, 80% at 6.25, 12.5, 25 mg/kg, respectively[1].
Ilorasertib (0, 3.75, 7.5, 15 mg/kg; i.p.) inhibits the histone H3 phosphorylation at 4-8 h in blood-borne tumor cells[2].
Ilorasertib (0.2 mg/kg; i.v.) shows anti-VEGF activity in mouse[2].
Ilorasertib (20 mg/kg; p.o.;once weekly for 3 weeks) shows anti-tumor activity in mouse[2].

Animal Model:Female SCID/beige mice[2]
Dosage:25 mg/kg
Administration:Subcutaneous minipump; 24 h
Result:Inhibited the histone H3 phosphorylation and the tumor drug concentration associated with 50% inhibition of histone H3 phosphorylation.
Animal Model:22-26 g, female NOD/SCID mice (xenograft model of multiple myeloma (KMS11))[2]
Dosage:20 mg/kg
Administration:P.o.; once weekly for 3 weeks
Result:Inhibited the tumor growth in mouse.
Clinical Trial
分子量

488.54

性状

Solid

Formula

C25H21FN6O2S

CAS 号

1227939-82-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 41.67 mg/mL(85.29 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0469 mL10.2346 mL20.4692 mL
5 mM0.4094 mL2.0469 mL4.0938 mL
10 mM0.2047 mL1.0235 mL2.0469 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.26 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: 2.08 mg/mL (4.26 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.26 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。