1. PROTAC Protein Tyrosine Kinase/RTK
  2. PROTACs FLT3
  3. PF15

PF15 是由 FLT3 kinase 配体和 CRBN 配体相连的 PROTAC,是一种具有高选择性的 FLT3-ITD 降解剂,其 DC50 值为 76.7 nM。PF15 能显著抑制 FLT3-ITD 阳性细胞的增殖,下调 FLT3STAT5 的磷酸化。PF15 还能抑制小鼠模型中肿瘤的生长,可用于白血病的研究。

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PF15 Chemical Structure

PF15 Chemical Structure

CAS No. : 2892631-70-6

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PF15 的其他形式现货产品:

Customer Review

Other Forms of PF15:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia[1].

体外研究
(In Vitro)

PF15 (0-1000 nM; 72 h) shows good anti-proliferation activity in MV4-11, Molm-13 and BaF3 cells (transformed ITD, ITD-D835V, and ITD-F691L mutations)[1].
PF15 (1, 3, 10, 30, 100, 300, 1000 nM; 6 h) obviously induces FLT3 degradation in a dose-dependent manner and (10, 30, 100, 300, 1000 nM; 6 h) dramatically inhibits the phosphorylation of FLT3 and STAT5 in BaF3-FLT3-ITD cells[1].
PF15 (10, 30, 100, 300, 1000 nM; 6 h) sharply downregulates the phosphorylation of FLT3 and STAT5 at 100 nM in both BaF3-FLT3-ITD-D835V and BaF3-FLT3-ITD-F691L cells[1].
PF15 (100 nM; 1, 3, 6, 12, 24 h) induces FLT3 degradation in a time-dependent manner from 1 h to 24 h[1].
PF15 (15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM; 24 h) induces FLT3 degradation with a DC50 of 76.7 nM[1].

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

Cell Proliferation Assay[1]

Cell Line: MV4-11, Molm-13, BaF3 cells (transformed ITD, ITD-D835V, and ITD-F691L mutations)
Concentration: 0-1000 nM
Incubation Time: 72 h
Result: Exhibited anti-proliferation activity with IC50s of 4.83 nM (MV4-11), 4.01 nM (Molm-13) and 7.85, 120.1, 116.6 nM (for transformed BaF3 cells harboring ITD, ITD-D835V, and ITD-F691L mutations respectively).

Western Blot Analysis[1]

Cell Line: BaF3-FLT3-ITD, BaF3-FLT3-ITD-D835V, BaF3-FLT3-ITD-F691L cells
Concentration: 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 6 h
Result: Induced FLT3 degradation when at 3 nM and in a dose-dependent manner in BaF3-FLT3-ITD cells.
Dramatically inhibited the phosphorylation of FLT3 and STAT5 when concentration up to 30 nM in BaF3-FLT3-ITD cells, and at 100 nM in both BaF3-FLT3-ITD-D835V and BaF3-FLT3-ITD-F691L cells.

Western Blot Analysis[1]

Cell Line: BaF3-FLT3-ITD cells
Concentration: 100 nM
Incubation Time: 1, 3, 6, 12, 24 h
Result: Significantly induced FLT3 degradation in a time-dependent manner, and FLT3 completely degraded when at 24 h.

Western Blot Analysis[1]

Cell Line: BaF3-FLT3-ITD cell
Concentration: 15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM
Incubation Time: 24 h
Result: Notably induced FLT3 degradation when at 125 nM, and DC50 was 76.7 nM.
体内研究
(In Vivo)

PF15 (10 or 20 mg/kg; i.p.; once daily for 10 days) shows good tumor growth inhibition with an inhibitory rate of 58.4% at dosage of 10 mg/kg, and when up to 20 mg/kg displays higher inhibitory rate[1].
PF15 (twice daily (20 mg/kg), once daily (40 mg/kg); 12 days; i.p.) prolongs the median survival up to 15 days (negative control group is 11 days) in BaF3-FLT3-ITD in situ model[1].

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

Animal Model: Female NOD/SCID mice (BaF3-FLT3-ITD xenograft model)[1].
Dosage: 10 or 20 mg/kg
Administration: Intraperitoneal injection; once daily for 10 days.
Result: Achieved good tumor growth inhibition with an inhibitory rate of 58.4% (10 mg/kg), meanwhile, when at 20 mg/kg displayed higher inhibitory rate.
Hardly caused side effects on heart, liver, and kidney (both of the treatment groups).
Animal Model: Female BALB/c nude mice (BaF3-FLT3-ITD in situ model)[1].
Dosage: 20, 40 mg/kg
Administration: Intraperitoneal injection; twice daily (20 mg/kg), once daily (40 mg/kg); 12 days.
Result: Prolonged the median survival from 11days to 15 days (both of the treatment groups).
分子量

855.94

Formula

C44H49N13O6

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (116.83 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1683 mL 5.8415 mL 11.6831 mL
5 mM 0.2337 mL 1.1683 mL 2.3366 mL
查看完整储备液配制表
  • 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 (2.92 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.92 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,此方案实验周期在半个月以上的动物实验酌情使用。

    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。

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

完整储备液配制表

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1683 mL 5.8415 mL 11.6831 mL 29.2077 mL
5 mM 0.2337 mL 1.1683 mL 2.3366 mL 5.8415 mL
10 mM 0.1168 mL 0.5842 mL 1.1683 mL 2.9208 mL
15 mM 0.0779 mL 0.3894 mL 0.7789 mL 1.9472 mL
20 mM 0.0584 mL 0.2921 mL 0.5842 mL 1.4604 mL
25 mM 0.0467 mL 0.2337 mL 0.4673 mL 1.1683 mL
30 mM 0.0389 mL 0.1947 mL 0.3894 mL 0.9736 mL
40 mM 0.0292 mL 0.1460 mL 0.2921 mL 0.7302 mL
50 mM 0.0234 mL 0.1168 mL 0.2337 mL 0.5842 mL
60 mM 0.0195 mL 0.0974 mL 0.1947 mL 0.4868 mL
80 mM 0.0146 mL 0.0730 mL 0.1460 mL 0.3651 mL
100 mM 0.0117 mL 0.0584 mL 0.1168 mL 0.2921 mL
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  • 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.

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产品名称:
PF15
目录号:
HY-143286
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