标签归档：flt

FLT3-IN-4

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FLT3-IN-4 

FLT3-IN-4 是一种口服有效的 Fms 样酪氨酸受体激酶 3 (FLT3; IC50= 7 nM) 抑制剂，可用于急性髓性白血病的研究。

FLT3-IN-4

FLT3-IN-4 Chemical Structure

CAS No. : 2304799-09-3

规格 价格 是否有货
5 mg ￥4800 询问价格 & 货期
10 mg ￥8000 询问价格 & 货期
25 mg ￥15500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia[1].

体外研究
(In Vitro)

FLT3-IN-4 (Compound 9u) shows potent inhibitory activities against MV4-11 and Molm-13 cells with IC50 values are 0.089±0.001 nM and 0.022±0.003 nM, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

431.49

Formula

C23H25N7O2
CAS 号

2304799-09-3
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.
参考文献

  • [1]. Yuan X, et al. Identification of Pyrrolo[2,3- d]pyrimidine-Based Derivatives as Potent and Orally Effective Fms-like Tyrosine Receptor Kinase 3 (FLT3) Inhibitors for Treating Acute Myelogenous Leukemia. J Med Chem. 2019 Apr 25;62(8):4158-4173.

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Quizartinib(Synonyms: 奎扎替尼; AC220)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Quizartinib (Synonyms: 奎扎替尼; AC220) 纯度: 98.87%

Quizartinib (AC220) 是一种具有口服活性的、高选择性的，有效的第二代 Ⅱ 型 FLT3 (type II FLT3) 酪氨酸激酶抑制剂，Kd 值为 1.6 nM。Quizartinib 抑制 Wt FLT3 和 突变型 FLT3-ITD 自磷酸化，IC50 分别为 4.1 nM 和 1.1 nM。Quizartinib 可以通过优化的 linker 与 VHL 配体连接，从而形成 PROTAC Flt3 降解剂。Quizartinib 诱导细胞凋亡 (apoptosis)。

Quizartinib(Synonyms: 奎扎替尼; AC220)

Quizartinib Chemical Structure

CAS No. : 950769-58-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1172 In-stock
5 mg ￥950 In-stock
10 mg ￥1550 In-stock
50 mg ￥4200 In-stock
100 mg ￥7200 In-stock
200 mg ￥9950 In-stock
500 mg ￥19500 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Quizartinib 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Drug Repurposing Compound Library
  • Covalent Screening Library
  • Orally Active Compound Library
  • Chemical Probe Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Blood Cancer Compound Library
  • Rare Diseases Drug Library

生物活性

Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis[1].

IC50 & Target

Kd: 1.6±0.7 nM (Flt3)[1]
体外研究
(In Vitro)

Quizartinib (AC220) is a novel compound expressly optimized as a FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). Quizartinib inhibits FLT3-WT and FLT3-ITD autophosphorylation with IC50 of 4.2±0.3 nM and 1.1±0.1 nM, respectively. Quizartinib inhibits MV4-11 and A375 cells with IC50 of 0.56±0.3 nM and >10 000 nM, respectively. Quizartinib inhibits FLT3 with low nanomolar potency in cellular assays and is highly selective when screened against the majority of the human protein kinome[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Quizartinib (AC220) inhibits FLT3 activity in vivo, significantly extends survival in a mouse model of FLT3-ITD AML at doses as low as 1 mg/kg when dosed orally once a day, eradicates tumors in a FLT3-dependent mouse xenograft model at 10 mg/kg, and potently inhibits FLT3 activity in primary patient cells. The oral bioavailability of Quizartinib, determined in rats by comparing oral and intravenous pharmacokinetics at 3 mg/kg, is approximately 40%. A single 10 mg/kg dose of Quizartinib is administered by oral gavage, and mice are killed at 2 time points after dosing, using groups of 4 animals each. Quantitation of total FLT3 and phospho-FLT3 in tumor samples revealed time-dependent inhibition of FLT3 autophosphorylation. FLT3 activity is inhibited by 90% at 2 hours, and 40% at 24 hours after administration. The extent of inhibition therefore correlated well with the expected free Quizartinib plasma levels, based on pharmacokinetic experiments[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

560.67

Formula

C29H32N6O4S
CAS 号

950769-58-1
中文名称

奎扎替尼
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 33 mg/mL (58.86 mM)

* “≥” 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 1.7836 mL 8.9179 mL 17.8358 mL
5 mM 0.3567 mL 1.7836 mL 3.5672 mL
10 mM 0.1784 mL 0.8918 mL 1.7836 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:
  • 1.

    Quizartinib (AC220) is prepared in vehicle (22% hydroxypropyl-β-cyclodextrin in sterile water)[2].
参考文献

  • [1]. Zarrinkar PP, et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood, 2009, 114(14), 2984-2992.

    [2]. Puissant A, et al. SYK is a critical regulator of FLT3 in acute myeloid leukemia. Cancer Cell. 2014 Feb 10;25(2):226-42.

    [3]. Sun X, et al. PROTACs: great opportunities for academia and industry. Signal Transduct Target Ther. 2019 Dec 24;4:64.
Kinase Assay
[1]

KinomeScan kinase binding assays are performed. For the FLT3 assay, a kinase construct that spanned the catalytic domain only (amino acids 592 to 969) is used. This construct does not include the juxtamembrane domain and is designed to measure the intrinsic binding affinity of the open FLT3 active site for inhibitors[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

MV4-11 and RS4;11 cells are cultured in Iscove media with 10% fetal bovine serum (FBS) and RPMI complete with 10% FBS, respectively. For proliferation assays, cells are cultured overnight in low serum media (0.5% FBS), then seeded in a 96-well plate at 40 000 cells per well. Inhibitors (e.g., Quizartinib) are added to the cells and incubated at 37°C for 72 hours. Cell viability is measured using the Cell Titer-Blue Cell Viability Assay. To measure inhibition of FLT3 autophosphorylation, cells are cultured in low serum media (0.5% FBS) overnight and seeded at a density of 400 000 cells per well in a 96-well plate the following day. The cells are incubated with inhibitors (e.g., Quizartinib) for 2 hours at 37°C. To induce FLT3 autophosphorylation in RS4;11 cells, 100 ng/mL FLT3 ligand is added for 15 minutes after the 2-hour compound incubation. Cell lysates are prepared and incubated in 96-well plates precoated with a total FLT3 capture antibody. The coated plates are incubated with either a biotinylated antibody against FLT3 to detect total FLT3 or an antibody against phosphotyrosines to detect FLT3 autophosphorylation. In both cases, a SULFO-tagged streptavidin secondary antibody is used for electrochemiluminescence detection on the Meso Scale Discovery platform[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Female NU/NU or severe combined immunodeficient mice are used. Quizartinib (hydrochloride salt) is formulated in 22% hydroxypropyl-β-cyclodextrin, CEP-701 is formulated in 20% gelucire 44/14 in water (vol/vol), MLN-518 and SU 11248 are formulated in 10 mM sodium citrate (pH 3.5), PKC-412 is formulated in 3:1 gelucire 44/14-propylene glycol (vol/vol), and Bay 43-9006 is formulated in 80% PEG-400. Compound concentrations are chosen to deliver the desired dose in a volume of 10 mL/kg. Compounds are administered by oral gavage and plasma samples collected 0.25, 0.5, 1, 2, 4, 6, and 24 hours after dosing. To collect plasma samples, eye bleeds (150 μL) are taken semilongitudinally using 3 groups of 3 animals each, taking 2 to 3 time points per animal to obtain a total of 3 independent plasma concentration time courses. Plasma samples and controls (25 μL) are extracted with 4 volumes of acetonitrile containing an internal standard and analyzed by liquid chromatography tandem mass spectrometry.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Zarrinkar PP, et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood, 2009, 114(14), 2984-2992.

    [2]. Puissant A, et al. SYK is a critical regulator of FLT3 in acute myeloid leukemia. Cancer Cell. 2014 Feb 10;25(2):226-42.

    [3]. Sun X, et al. PROTACs: great opportunities for academia and industry. Signal Transduct Target Ther. 2019 Dec 24;4:64.

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

FLT3-IN-10

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FLT3-IN-10 

FLT3-IN-10 (compound 7c) 是 FMS 样酪氨酸激酶 3 (FLT3) 的有效抑制剂。FLT3-IN-10 具有治疗 FLT3 突变的急性髓性白血病 (AML) 的潜力。

FLT3-IN-10

FLT3-IN-10 Chemical Structure

CAS No. : 2088735-51-5

规格 价格 是否有货
5 mg ￥1800 询问价格 & 货期
10 mg ￥3000 询问价格 & 货期
25 mg ￥6200 询问价格 & 货期
50 mg ￥9800 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

FLT3-IN-10 (compound 7c) is a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3). FLT3-IN-10 has the potential for the treatment of FLT3-mutated acute myeloid leukemia (AML)[1].

IC50 & Target

FLT3[1]
分子量

254.26

Formula

C15H11FN2O
CAS 号

2088735-51-5
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.
参考文献

  • [1]. Kim HJ, et al. Discovery of Oxazol-2-amine Derivatives as Potent Novel FLT3 Inhibitors. Molecules. 2020;25(21):5154.

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PROTAC FLT-3 degrader 1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PROTAC FLT-3 degrader 1  纯度: 98.70%

PROTAC FLT-3 degrader 1 是基于 von Hippel-Lindau 的 FLT-3内部串联重复 (ITD) 降解剂 PROTAC，IC50为0.6 nM。抗增殖，诱导凋亡活性。

PROTAC FLT-3 degrader 1

PROTAC FLT-3 degrader 1 Chemical Structure

CAS No. : 2230826-81-8

规格 价格 是否有货 数量
1 mg ￥7800 In-stock
5 mg ￥20000 In-stock
10 mg ￥32000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

PROTAC FLT-3 degrader 1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

PROTAC FLT-3 degrader 1 is a von Hippel-Lindau-based PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction[1].

IC50 & Target

IC50: 0.6 nM (FLT-3 ITD)[1]
分子量

1020.23

Formula

C52H61N9O9S2
CAS 号

2230826-81-8
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 150 mg/mL (147.03 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9802 mL 4.9009 mL 9.8017 mL
5 mM 0.1960 mL 0.9802 mL 1.9603 mL
10 mM 0.0980 mL 0.4901 mL 0.9802 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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: 7.5 mg/mL (7.35 mM); Suspended solution; Need ultrasonic

    此方案可获得 7.5 mg/mL (7.35 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 75.0 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-CD in saline)

    Solubility: 7.5 mg/mL (7.35 mM); Suspended solution; Need ultrasonic

    此方案可获得 7.5 mg/mL (7.35 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 75.0 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。

    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: ≥ 7.5 mg/mL (7.35 mM); Clear solution

    此方案可获得 ≥ 7.5 mg/mL (7.35 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 75.0 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Burslem GM, et al. Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion. J Am Chem Soc. 2018 Dec 5;140(48):16428-16432.

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

FLT3-IN-6

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FLT3-IN-6  纯度: 99.14%

FLT3-IN-6 是一种有效、选择性的 FLT3-ITD (FLT3 突变体) 抑制剂，IC50 值为 1.336 nM。

FLT3-IN-6

FLT3-IN-6 Chemical Structure

CAS No. : 2377141-31-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3850 In-stock
5 mg ￥3500 In-stock
10 mg ￥5800 In-stock
25 mg ￥11000 In-stock
50 mg ￥17000 In-stock
100 mg ￥25000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

FLT3-IN-6 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

FLT3-IN-6 is a potent and selective inhibitor of FLT3-ITD (FLT3 mutation) with an IC50 of 1.336 nM[1].

IC50 & Target

IC50: 1.336 nM (FLT3-ITD)[1]
分子量

419.48

Formula

C23H25N5O3
CAS 号

2377141-31-4
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (595.98 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3839 mL 11.9195 mL 23.8390 mL
5 mM 0.4768 mL 2.3839 mL 4.7678 mL
10 mM 0.2384 mL 1.1920 mL 2.3839 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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 (4.96 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.96 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-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.96 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.96 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 900 μL 20% 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: ≥ 2.08 mg/mL (4.96 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.96 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 20.8 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Heng H, et al. Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model. Eur J Med Chem. 2019 Aug 15;176:248-267.

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

美国Axygen 96孔PCR板PCR-96-C/PCR-96-FLT-C/PCR-96-FLT-C

发表于由

【简单介绍】

美国Axygen 96孔PCR板PCR-96-C/PCR-96-FLT-C/PCR-96-FLT-C/PCR-96-AB-C，

金畔生物科技 量多优惠

【详细说明】

美国Axygen 96孔PCR板PCR-96-C/PCR-96-FLT-C/PCR-96-FLT-C/PCR-96-AB-C

名称：96孔PCR板

品牌：美国AXYGEN

美国Axygen 96孔PCR板PCR-96-C/PCR-96-FLT-C/PCR-96-FLT-C/PCR-96-AB-C

订货号：

PCR-96-AB-C

96孔PCR板（ABI）

10块/5包/箱

包

PCR-96-C

96孔PCR板（无裙边）

10块/5包/箱

包

PCR-96-FLT-C

96孔平顶PCR板

5*5块/4包/箱

包

PCR-96-LP-FLT-C

96孔低位平顶PCR板（0.1ml）

5*5块/4包/箱

包

PCR-96-FS-C

96孔全裙透明PCR板

 10块/5包/箱

包

PCR-96-SG-C

96孔PCR板（裙边分段）

10块/5包/箱

包

PCR-96-LP-AB-C

96孔低位PCR板（0.1ml）

5*5块/4包/箱

包

AM-96-PCR-RD

96孔PCR板的密封盖

10个/5包/箱

包

PCR-96M2-HS-C-NP

半裙96孔PCR板（无色透明）

10块/5包/箱

包

PCR-96M2-HS-C

半裙96孔PCR板（黑色编号）

10块/5包/箱

包

PCR-96M2-HS-W

半裙96孔PCR板（白色）

10块/5包/箱

包

PCR-96M2-HS-BK

半裙96孔PCR板（黑色）

10块/5包/箱

包

/PCR-96-AB-C

JAK2/FLT3-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

JAK2/FLT3-IN-1 

JAK2/FLT3-IN-1 是一种口服有效的双重 JAK2/FLT3 抑制剂，对 JAK2，FLT3，JAK1 和 JAK3 的 IC50 分别为 0.7 nM，4 nM，26 nM 和 39 nM。JAK2/FLT3-IN-1 具有抗癌活性。

JAK2/FLT3-IN-1

JAK2/FLT3-IN-1 Chemical Structure

CAS No. : 2387765-27-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

JAK2/FLT3-IN-1 的其他形式现货产品:

JAK2/FLT3-IN-1 TFA

生物活性

JAK2/FLT3-IN-1 is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity[1].

IC50 & Target[1]

JAK2

0.7 nM (IC50)

FLT3

4 nM (IC50)

JAK1

26 nM (IC50)

JAK3

39 nM (IC50)

体外研究
(In Vitro)

JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) down-regulates p-FLT3 in a dose-dependent manner[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MV4-11 and SET-2 cells
Concentration: 0.008, 0.04, 0.2, 1 μM
Incubation Time: For 2 hours
Result: Down-regulated p-FLT3 in a dose-dependent manner from 0.008 to 1 μM.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 50, 100 nM
Incubation Time: For 2 hours
Result: Had a dose-dependent effect on the induction of apoptosis in the MV4-11 cells.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5, 10, 50, 100 nM
Incubation Time: For 2 hours
Result: Induced cell cycle arrest with a G1/G0 percentage of 85% at 100 nM.

体内研究
(In Vivo)

JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) exhibits significant antitumor effects[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD/SCID mouse models[1]
Dosage: 30 and 60 mg/kg
Administration: Oral administration; daily; for 14 days
Result: Exhibited significant antitumor effects.
The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.

分子量

467.58

Formula

C25H34FN7O
CAS 号

2387765-27-5
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
In Vitro: 

DMSO : 20.83 mg/mL (44.55 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1387 mL 10.6934 mL 21.3867 mL
5 mM 0.4277 mL 2.1387 mL 4.2773 mL
10 mM 0.2139 mL 1.0693 mL 2.1387 mL

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 (4.45 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.45 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 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-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.45 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.45 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 900 μL 20% 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Yang T, et al. Discovery of Potent and Orally Effective Dual JAK2/FLT3 Inhibitors for the Treatment of AcuteMyelogenous Leukemia and Myeloproliferative Neoplasms. J Med Chem. 2019 Oct 31.

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