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ENMD-2076
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。
ENMD-2076图片
CAS NO:934353-76-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
ENMD-2076是多靶点激酶抑制剂,抑制Aurora AFlt3KDR/VEGFR2Flt4/VEGFR3FGFR1FGFR2SrcPDGFRαIC50值分别为1.86,14,58.2,15.9,92.7,70.8,20.2 and 56.4 nM。
生物活性

ENMD-2076 is a multi-targeted kinase inhibitor withIC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM forAurora A,Flt3,KDR/VEGFR2,Flt4/VEGFR3,FGFR1,FGFR2,Src,PDGFRα, respectively.

IC50& Target[1]

Aurora A

14 nM (IC50)

KDR

58.2 nM (IC50)

Flt-4

15.9 nM (IC50)

FGFR1

92.7 nM (IC50)

FGFR2

70.8 nM (IC50)

PDGFRα

56.4 nM (IC50)

Flt3

1.86 nM (IC50)

体外研究
(In Vitro)

ENMD-2076 is selective toward Aurora A versus Aurora B (IC50=350 nM). ENMD-2076 inhibits HUVEC growth with an IC50value of 0.15 mM. Against 10 human leukemia cell lines, the IC50values range from 0.025 to 0.53 mM. Within this panel, MV4:11 cells are the most sensitive cells by a factor of greater than 4. The lymphoma-derived U937 cell line treated with ENMD-2076 shows that the ENMD-2076 induces a dose-dependent increase in G2-M-phase arrest as well as the induction of apoptosis. ENMD-2076 inhibits cellular Flt3 ligand (FL)-induced Flt3 autophosphorylation in THP-1 cells, which have been shown to express FL-responsive wild-type Flt- 3 (18) with an IC50value of 28 nM. ENMD-2076 inhibits stem cell factor (SCF)-induced Kit autophosphorylation in MO7e cells with an IC50value of 40 nM. ENMD-2076 inhibits VEGFR2/KDR autophosphorylation with an IC50value of 7 nM[1].

体内研究
(In Vivo)

ENMD-2076 treatment results in statistically significant, dose dependent inhibition of tumor growth or tumor regression. Moreover, there is no correlation between tumor growth rate and antitumor efficacy, which would conceivably be expected for a mitotic kinase inhibitor, as fast growing (e.g., A375 melanoma) and slow-growing (e.g., HT29 colon carcinoma) tumors are similarly inhibited by ENMD-2076. ENMD-2076 is well tolerated at daily doses up to 302 mg/kg (equivalent to 200 mg/kg of the free base), with no weight loss or signs of morbidity noted in any study at this dose with the exception of the A375 model[1].

Clinical Trial
分子量

375.47

性状

Solid

Formula

C21H25N7

CAS 号

934353-76-1

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 : ≥ 31 mg/mL(82.56 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6633 mL13.3166 mL26.6333 mL
5 mM0.5327 mL2.6633 mL5.3267 mL
10 mM0.2663 mL1.3317 mL2.6633 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: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.66 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: 2.5 mg/mL (6.66 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.66 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 25.0 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.66 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。