1. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK
  2. CDK FLT3
  3. FN-1501

FN-1501 是一种有效的 FLT3CDK 抑制剂,对 CDK2/cyclin A,CDK4/cyclin D1,CDK6/cyclin D1 和 FLT3IC50 值分别为 2.47,0.85,1.96, 和 0.28 nM。FN-1501 具有抗肿瘤的活性。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

FN-1501 Chemical Structure

FN-1501 Chemical Structure

CAS No. : 1429515-59-2

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1633
In-stock
1 mg ¥780
In-stock
5 mg ¥1720
In-stock
10 mg ¥2583
In-stock
25 mg ¥4650
In-stock
50 mg ¥6975
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.

IC50 & Target[1]

Cdk4/cyclin D1

0.85 nM (IC50)

CDK6/cyclinD1

1.96 nM (IC50)

cdk2/cyclin A

2.47 nM (IC50)

FLT3

0.28 nM (IC50)

体外研究
(In Vitro)

FN-1501 是一种有效的 FLT3CDK 抑制剂,对 CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 以及 FLT3 的 IC50 值分别为 2.47 ± 0.21、0.85 ± 0.28、1.96 ± 0.08 和 0.28 ± 0.01 nM。FN-1501 对 MGC803、RS4 11、MCF-7、HCT-116 和 NCI-H82 等多种肿瘤细胞显示出有效的抑制活性,GI50 分别为 0.37 ± 0.04、0.05 ± 0.01、2.84 ± 0.25、0.09 ± 0.04、0.11 ± 0.02 nM[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

FN-1501 具有强效的抗肿瘤活性,对正常淋巴细胞几乎没有细胞毒性,在 ICR 小鼠中的 LD50 为 185.67 mg/kg。FN-1501 (15. 30,或 40 mg/kg/d,iv) 剂量依赖性抑制 MV4-11 细胞异种移植小鼠中肿瘤的生长[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

431.49

Formula

C22H25N9O

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 50 mg/mL (115.88 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3176 mL 11.5878 mL 23.1755 mL
5 mM 0.4635 mL 2.3176 mL 4.6351 mL
查看完整储备液配制表

* 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°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

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

    Solubility: ≥ 2.5 mg/mL (5.79 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.79 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Kinase Assay
[1]

The activity of the CDKs and FLT3 are assayed in reaction buffer (20 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, 1% DMSO) at room temperature at a final ATP concentration of 10 mM. Then FLT3, dissolved in 100% DMSO at the indicated doses, are delivered into the kinase reaction mixture by acoustic technology and incubated for 20 min at room temperature. After 10 μM [γ-33P] ATP (specific activity 10 Ci/μL) is added to initiate the reaction, the reactions are carried out at 25°C for 120 min. The kinase activities are detected by the filterbinding method. IC50 values and curve fits are obtained by Prism[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

The human AML cell line MV4-11 is cultured in IMDM media with 10% FBS and supplemented with 2% l-glutamine and 1% penicillin/streptomycin. The MV4-11 cell line is maintained in culture media at 37°C with 5% CO2. The effects of FN-1501 on MV4-11 proliferation are performed. Cells are cultured in 96-well culture plates (10 000 cells/well). FN-1501 at various concentrations is added to the plates. Cell proliferation is determined after treatment with FN-1501 for 72 h. Cell viability is measured using the CellTiter-Glo assay, and luminescence is measured in a multilabel reader. Data are normalized to control groups (DMSO) and represented as the means of three independent measurements with standard errors of <20%. IC50 values are calculated using Prism 5.0[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Six-week-old female nu/nu mice are housed in a specific pathogen-free facility. Prior to implantation, cells are harvested during exponential growth. Five million MV4-11 cells in PBS are formulated as a 1:1 mixture with a Matrigel and injected into the subcutaneous space on the right flank of each nu/nu mouse. Daily intravenous injections are initiated when MV4-11 tumors have reached sizes of 100-200 mm3. The animals are then randomized into treatment groups of 8 mice each for the efficacy studies and dosed with FN-1501 (0, 15, 30, or 40 (mg/kg)/d) or cytarabine (50 (mg/kg)/d). The compounds (FN-1501, etc.) are dissolved in a solution of PEG400 (25%), ethanol (3.7%), glucose (5%), and acetic acid/sodium acetate buffer (pH 4.5, 7.5%). Tumor growth is measured every 3 days using Vernier calipers for the duration of the treatment. The volume is calculated as follows: tumor volume = a × b2/2, where a is the long diameter, and b is the short diameter. The percentage of tumor-growth inhibition (GI) is calculated as follows: GI = 100% × {1 - [(tumor volumefinal - tumor volumeinitial for the compound-treated group)/(tumor volumefinal - tumor volumeinitial for the vehicle-treated group)]}. The percent tumor regression (PTR) is calculated as follows: PTR = 100% × (tumor volumeinitial - tumor volumefinal)/(tumor volumeinitial)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 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°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3176 mL 11.5878 mL 23.1755 mL 57.9388 mL
5 mM 0.4635 mL 2.3176 mL 4.6351 mL 11.5878 mL
10 mM 0.2318 mL 1.1588 mL 2.3176 mL 5.7939 mL
15 mM 0.1545 mL 0.7725 mL 1.5450 mL 3.8626 mL
20 mM 0.1159 mL 0.5794 mL 1.1588 mL 2.8969 mL
25 mM 0.0927 mL 0.4635 mL 0.9270 mL 2.3176 mL
30 mM 0.0773 mL 0.3863 mL 0.7725 mL 1.9313 mL
40 mM 0.0579 mL 0.2897 mL 0.5794 mL 1.4485 mL
50 mM 0.0464 mL 0.2318 mL 0.4635 mL 1.1588 mL
60 mM 0.0386 mL 0.1931 mL 0.3863 mL 0.9656 mL
80 mM 0.0290 mL 0.1448 mL 0.2897 mL 0.7242 mL
100 mM 0.0232 mL 0.1159 mL 0.2318 mL 0.5794 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
FN-1501
目录号:
HY-111361
需求量: