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生物活性分子抑制剂E7046

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。
E7046  纯度: 99.68%

E7046 是一种口服有效的，特异性的 EP4 拮抗剂，IC50 值为 13.5 nM， Ki 值为 23.14 nM；E7046 具有抗肿瘤活性。

E7046

E7046 Chemical Structure

CAS No. : 1369489-71-3

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 ￥550 In-stock
5 mg ￥500 In-stock
10 mg ￥700 In-stock
25 mg ￥1300 In-stock
50 mg ￥2300 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

E7046 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Endocrinology Compound Library
  • Orally Active Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library

生物活性

E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. E7046 exhibits anti-tumor activities[1][2].

IC50 & Target[2]

EP4

13.5 nM (IC50)

EP4

23.14 nM (Ki)

体外研究
(In Vitro)

E7046 reverses the immunosuppressive effects of PGE2 on activation and differentiation of human myeloid cells through selective EP4 antagonism[2].

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)

In the CT-26 tumor model, the E7046/RT combination causes the anti-tumor memory response of 9 animals. In the 4T1 model, the combination of E7046 and RT also produces significant better tumor growth inhibition activity compared with each treatment alone. The combination significantly improves survival by inhibiting the subsequent spontaneous lung metastasis of 4T1 tumors[1]. E7046 (150 mg/kg) inhibits the growth of multiple syngeneic tumor models. Blockade of EP4 signaling promotes anti-tumor DC differentiation and slows tumor growth in mice. E7046 treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8C T cells. Furthermore, co-administration of E7046 and E7777, an IL-2-diphtheria toxin fusion protein that preferentially kills Tregs, synergistically disrupts the myeloid and Treg immunosuppressive networks, resulting in effective and durable anti-tumor immune responses in mouse tumor models[2].

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

483.39

Formula

C22H18F5N3O4
CAS 号

1369489-71-3
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 : ≥ 100 mg/mL (206.87 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 2.0687 mL 10.3436 mL 20.6872 mL
5 mM 0.4137 mL 2.0687 mL 4.1374 mL
10 mM 0.2069 mL 1.0344 mL 2.0687 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 (4.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.30 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 (4.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.30 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 (4.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.30 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. X. Bao, et al. Combination of a Novel EP4 Antagonist E7046 and Radiation Therapy Promotes Anti-tumor Immune Response and Tumor Rejection in Preclinical Tumor Models. International Journal of Radiation Oncology Biology Physics

    [2]. Diana I. Albu, et al. EP4 Antagonism by E7046 diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity. OncoImmunology.
Cell Assay
[2]

Bone marrow (BM) cells are flushed from femurs of BALB/c mice using sterile CM. Freshly harvested (BM) cells (0.5×106) are differentiated in the presence of 20 ng/mL recombinant mouse GM-CSF, ±PGE2 (10 nM), at 37°C, for 8 d. CM C fresh GM-CSF ± PGE2 is changed on days 3 and 6. After in vitro differentiation, cells are analyzed by flow cytometry. For certain experiments, CT26, 4T1 cell supernatants, and/or EP1 (SC-57089), EP2 (ER-880696), EP3 (L-798106), or EP4 (E7046) antagonists at 1 mM, are added to the BM cells. To assess the effect of differentiated BM cells on T cell proliferation, mouse BM cells differentiated are co-cultured for 72 hours with anti-CD3/CD28 Dynabeadsstimulated and CFSE (1 mM)-stained T cells. T cell proliferation is assessed by CFSE dilution using flow cytometry.

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
[2]

For the tumor isograft efficacy studies, 6-week old female BALB/c mice are implanted with cancer cells: 1×105 CT26 or 4T1 cells or 8×105 H22 cells per mouse s.c., or 1×105 EMT6 cells in the mammary fat pad. C57BL/6 mice are implanted s.c. with 1×106 Pan02 cells per mouse, and A/J mice are implanted s.c. with 2-3 mm3 SAI/N tumor fragments. To investigate the role of T cells in the anti-tumor response, 6 week old female nude mice (which lack T cells) are injected s.c. with 1×105 CT26 cells. When tumors reach approximately 50-100 mm3, tumor-bearing mice are randomly assigned to vehicle or treatment groups, and treatment regimens begin. E7046 is administered per oral (p.o.) as a 100 or 150 mg/kg suspension in 0.5% MC, daily for 21 d (QDx21). For the combination studies, E7777 is administered intravenously (i.v.) at 2.5 mg/mouse in saline, as 2 to 3 doses injected one week apart (Q7Dx2-3). Tumor volumes and body weights are recorded 2-3 times a week. For comparison with current immunotherapies, in addition to vehicle control and E7046 C E7777 groups, mice are assigned to anti-PD1 antibodies or anti-mouse PD-1 C antimouse CTLA4 antibodies treatment groups. Anti-PD-1 and anti-CTLA-4 antibodies (1 mg/mL), are administered i.p. in 100 mL, 3 times 4 d apart (Q4Dx3) for a total of 300 mg each. Isotype controls are administered i.p. at 1 mg/mL to the control group. For the CD4CT and CD8CT lymphocyte depletion, antimouse CD4 or anti-mouse CD8 antibodies or their isotype controls are administered in 100 mL, i.p. at 2.5 mg/mL every 4 days, for a total of 4 injections per mouse (1 mg).

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]. X. Bao, et al. Combination of a Novel EP4 Antagonist E7046 and Radiation Therapy Promotes Anti-tumor Immune Response and Tumor Rejection in Preclinical Tumor Models. International Journal of Radiation Oncology Biology Physics

    [2]. Diana I. Albu, et al. EP4 Antagonism by E7046 diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity. OncoImmunology.

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

生物活性分子抑制剂E7046

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。

E7046  纯度: 99.68%

E7046 是一种口服有效的，特异性的 EP4 拮抗剂，IC50 值为 13.5 nM， Ki 值为 23.14 nM；E7046 具有抗肿瘤活性。

E7046

E7046 Chemical Structure

CAS No. : 1369489-71-3

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 ￥550 In-stock
5 mg ￥500 In-stock
10 mg ￥700 In-stock
25 mg ￥1300 In-stock
50 mg ￥2300 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

E7046 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Endocrinology Compound Library
  • Orally Active Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library

生物活性

E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. E7046 exhibits anti-tumor activities[1][2].

IC50 & Target[2]

EP4

13.5 nM (IC50)

EP4

23.14 nM (Ki)

体外研究
(In Vitro)

E7046 reverses the immunosuppressive effects of PGE2 on activation and differentiation of human myeloid cells through selective EP4 antagonism[2].

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)

In the CT-26 tumor model, the E7046/RT combination causes the anti-tumor memory response of 9 animals. In the 4T1 model, the combination of E7046 and RT also produces significant better tumor growth inhibition activity compared with each treatment alone. The combination significantly improves survival by inhibiting the subsequent spontaneous lung metastasis of 4T1 tumors[1]. E7046 (150 mg/kg) inhibits the growth of multiple syngeneic tumor models. Blockade of EP4 signaling promotes anti-tumor DC differentiation and slows tumor growth in mice. E7046 treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8C T cells. Furthermore, co-administration of E7046 and E7777, an IL-2-diphtheria toxin fusion protein that preferentially kills Tregs, synergistically disrupts the myeloid and Treg immunosuppressive networks, resulting in effective and durable anti-tumor immune responses in mouse tumor models[2].

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

483.39

Formula

C22H18F5N3O4
CAS 号

1369489-71-3
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 : ≥ 100 mg/mL (206.87 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 2.0687 mL 10.3436 mL 20.6872 mL
5 mM 0.4137 mL 2.0687 mL 4.1374 mL
10 mM 0.2069 mL 1.0344 mL 2.0687 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 (4.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.30 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 (4.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.30 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 (4.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.30 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. X. Bao, et al. Combination of a Novel EP4 Antagonist E7046 and Radiation Therapy Promotes Anti-tumor Immune Response and Tumor Rejection in Preclinical Tumor Models. International Journal of Radiation Oncology Biology Physics

    [2]. Diana I. Albu, et al. EP4 Antagonism by E7046 diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity. OncoImmunology.
Cell Assay
[2]

Bone marrow (BM) cells are flushed from femurs of BALB/c mice using sterile CM. Freshly harvested (BM) cells (0.5×106) are differentiated in the presence of 20 ng/mL recombinant mouse GM-CSF, ±PGE2 (10 nM), at 37°C, for 8 d. CM C fresh GM-CSF ± PGE2 is changed on days 3 and 6. After in vitro differentiation, cells are analyzed by flow cytometry. For certain experiments, CT26, 4T1 cell supernatants, and/or EP1 (SC-57089), EP2 (ER-880696), EP3 (L-798106), or EP4 (E7046) antagonists at 1 mM, are added to the BM cells. To assess the effect of differentiated BM cells on T cell proliferation, mouse BM cells differentiated are co-cultured for 72 hours with anti-CD3/CD28 Dynabeadsstimulated and CFSE (1 mM)-stained T cells. T cell proliferation is assessed by CFSE dilution using flow cytometry.

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
[2]

For the tumor isograft efficacy studies, 6-week old female BALB/c mice are implanted with cancer cells: 1×105 CT26 or 4T1 cells or 8×105 H22 cells per mouse s.c., or 1×105 EMT6 cells in the mammary fat pad. C57BL/6 mice are implanted s.c. with 1×106 Pan02 cells per mouse, and A/J mice are implanted s.c. with 2-3 mm3 SAI/N tumor fragments. To investigate the role of T cells in the anti-tumor response, 6 week old female nude mice (which lack T cells) are injected s.c. with 1×105 CT26 cells. When tumors reach approximately 50-100 mm3, tumor-bearing mice are randomly assigned to vehicle or treatment groups, and treatment regimens begin. E7046 is administered per oral (p.o.) as a 100 or 150 mg/kg suspension in 0.5% MC, daily for 21 d (QDx21). For the combination studies, E7777 is administered intravenously (i.v.) at 2.5 mg/mouse in saline, as 2 to 3 doses injected one week apart (Q7Dx2-3). Tumor volumes and body weights are recorded 2-3 times a week. For comparison with current immunotherapies, in addition to vehicle control and E7046 C E7777 groups, mice are assigned to anti-PD1 antibodies or anti-mouse PD-1 C antimouse CTLA4 antibodies treatment groups. Anti-PD-1 and anti-CTLA-4 antibodies (1 mg/mL), are administered i.p. in 100 mL, 3 times 4 d apart (Q4Dx3) for a total of 300 mg each. Isotype controls are administered i.p. at 1 mg/mL to the control group. For the CD4CT and CD8CT lymphocyte depletion, antimouse CD4 or anti-mouse CD8 antibodies or their isotype controls are administered in 100 mL, i.p. at 2.5 mg/mL every 4 days, for a total of 4 injections per mouse (1 mg).

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]. X. Bao, et al. Combination of a Novel EP4 Antagonist E7046 and Radiation Therapy Promotes Anti-tumor Immune Response and Tumor Rejection in Preclinical Tumor Models. International Journal of Radiation Oncology Biology Physics

    [2]. Diana I. Albu, et al. EP4 Antagonism by E7046 diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity. OncoImmunology.

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

RIPK1-IN-7

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。

RIPK1-IN-7  纯度: 98.67%

RIPK1-IN-7 是受体相互作用的蛋白激酶 1 (RIPK1) 抑制剂，Kd 值为 4 nM，IC50 值为 11 nM。RIPK1-IN-7 在实验性 B16 黑色素瘤肺转移模型中具有良好的抗转移活性。

RIPK1-IN-7

RIPK1-IN-7 Chemical Structure

CAS No. : 2300982-44-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4950 In-stock
5 mg ￥4500 In-stock
10 mg ￥7500 In-stock
50 mg ￥22500 In-stock
100 mg ￥33000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

RIPK1-IN-7 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • NF-κB Signaling Compound Library
  • Anti-Cancer Compound Library

生物活性

RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model[1].

IC50 & Target

IC50: 11 nM (RIPK1)[1]
Kd: 4 nM (RIPK1)[1]
体外研究
(In Vitro)

RIPK1-IN-7 shows potent cell protection effect in the TSZ-induced HT29 cell necroptosis model with an EC50 of 2nM[1].
RIPK1-IN-7 displays considerable activity against several other kinases, such as Flt4, TrkA, TrkB, TrkC, Axl, HRI, Mer, and MAP4K5 with IC50s of 20, 26, 8, 7, 35, 26, 29, and 27 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

481.47

Formula

C25H22F3N5O2
CAS 号

2300982-44-7
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 : 62.5 mg/mL (129.81 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0770 mL 10.3849 mL 20.7697 mL
5 mM 0.4154 mL 2.0770 mL 4.1539 mL
10 mM 0.2077 mL 1.0385 mL 2.0770 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 (4.32 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.32 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% corn oil

    Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.32 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Li Y, et al. Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model. J Med Chem. 2018 Dec 27;61(24):11398-11414.

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Kushenol E

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。

Kushenol E  纯度: ≥96.0%

Kushenol E 是从 Sophora flavescens 中分离出的一类类黄酮，是 IDO1 的非竞争性抑制剂，其 IC50 值为 7.7 µM，Ki 值为 9.5 µM，具有抗肿瘤活性。

Kushenol E

Kushenol E Chemical Structure

CAS No. : 99119-72-9

规格 价格 是否有货 数量
1 mg ￥3500 In-stock
5 mg ￥10500 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

Kushenol E 相关产品

•相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus

生物活性

Kushenol E is a class of flavonoids isolated from Sophora flavescens and is a non-competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 of 7.7 µM and a Ki of 9.5 µM, has anti-tumor activity[1].

分子量

424.49

Formula

C25H28O6
CAS 号

99119-72-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献

  • [1]. Kwon M, et al. Inhibitory effects of flavonoids isolated from Sophora flavescens on indoleamine 2,3-dioxygenase 1 activity. J Enzyme Inhib Med Chem. 2019 Dec;34(1):1481-1488.

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(R)-Trolox

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。

(R)-Trolox  纯度: 99.94%

(R)-Trolox 是维生素 E 类似物，是一种竞争性酪氨酸酶抑制剂，Ki 值为 0.83 mM，ID50 值为 1.88 mM。(R)-Trolox 具有比 (S) 对映异构体更强的酪氨酸酶亲和力 (Ki 值为 0.61 mM)。

(R)-Trolox

(R)-Trolox Chemical Structure

CAS No. : 53101-49-8

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 ￥550 In-stock
50 mg ￥500 In-stock
100 mg ￥850 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

(R)-Trolox 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library

生物活性

(R)-Trolox is a vitamin E analogue and a competitive tyrosinase inhibitor with a Ki value of 0.83 mM and a ID50 value of 1.88 mM[1]. The (R)-Trolox has stronger tyrosinase affinity than the (S) enantiomer (Ki value of 0.61 mM)[1].

体外研究
(In Vitro)

As compared to the control containing no inhibitor, DMSO suppresses the tyrosinase activity at tested levels, 100 and 200 µL in a total volume of 3.0 mL. The inhibition of DMSO on the mushroom tyrosinase is dosedependent. Additions of DMSO at the two levels in the tyrosinase digests containing (R)-Trolox ((R)-HTCCA) results in further inhibitions of the tyrosinase activity. The influence of the DMSO on the inhibitory effects of (R)-Trolox against the tyrosinase is also dose-dependent[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

250.29

Formula

C14H18O4
CAS 号

53101-49-8
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 : 250 mg/mL (998.84 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9954 mL 19.9768 mL 39.9537 mL
5 mM 0.7991 mL 3.9954 mL 7.9907 mL
10 mM 0.3995 mL 1.9977 mL 3.9954 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.25 mg/mL (8.99 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (8.99 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 22.5 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
  • 2.

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

    Solubility: ≥ 2.25 mg/mL (8.99 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (8.99 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 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (8.31 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.31 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

*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]. Yu L. Inhibitory effects of (S)- and (R)-6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acids on tyrosinase activity. J Agric Food Chem. 2003 Apr 9;51(8):2344-7.

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WIKI4

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。

WIKI4  纯度: 99.93%

WIKI4 是一种有效的 tankyrase 抑制剂，其对 TNKS2 的 IC50 值为 26 nM。WIKI4 有效抑制 Wnt/β-catenin 信号传导，其 EC50 值为 75 nM。WIKI4 通过抑制 TNKS2 的酶活性来介导其对 Wnt/β-catenin 信号传导的影响。WIKI4 对 SCLC 细胞具有细胞毒性，其 IC50 值为 0.02 μM。

WIKI4

WIKI4 Chemical Structure

CAS No. : 838818-26-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥688 In-stock
5 mg ￥600 In-stock
10 mg ￥920 In-stock
25 mg ￥1850 In-stock
50 mg ￥3300 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

WIKI4 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Cytoskeleton Compound Library
  • Neuroprotective Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Transcription Factor Targeted Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2[1][2]. WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM[3].

IC50 & Target[2]

TNKS2

26 nM (IC50)

体外研究
(In Vitro)

WIKI4 (100 nM, 1 μM; 6 days; DLD1 cells) inhibits growth of DLD1 cells relative to DMSO controls in media containing low serum. WIKI4 inhibits expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling[1].
WIKI4 (1 μM; 2 hours, 4 hours, 6 hours, or 24 hours; DLD1 cells) significantly increases the steady-state abundance of AXIN1 and AXIN2[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 Viability Assay[1]

Cell Line: DLD1 cells
Concentration: 100 nM, 1 μM
Incubation Time: 6 days
Result: Inhibited growth of DLD1 cells.

Western Blot Analysis[1]

Cell Line: DLD1 cells
Concentration: 1 μM
Incubation Time: 2 hours,4 hours,6 hours, or 24 hours
Result: Significantly increased the steady-state abundance of AXIN1 and AXIN2.

分子量

521.59

Formula

C29H23N5O3S
CAS 号

838818-26-1
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 : 6.8 mg/mL (13.04 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9172 mL 9.5861 mL 19.1721 mL
5 mM 0.3834 mL 1.9172 mL 3.8344 mL
10 mM 0.1917 mL 0.9586 mL 1.9172 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。
参考文献

  • [1]. James RG, et al. WIKI4, a novel inhibitor of tankyrase and Wnt/ß-catenin signaling. PLoS One. 2012;7(12):e50457.

    [2]. Haikarainen T, et al. Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4. PLoS One. 2013 Jun 6;8(6):e65404.

    [3]. Sadava D, et al. The effect of brassinolide, a plant steroid hormone, on drug resistant small-cell lung carcinoma cells. Biochem Biophys Res Commun. 2017 Nov 4;493(1):783-787.

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PF-5274857

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。

PF-5274857  纯度: 98.12%

PF-5274857 是一种有效的、选择性的、具有口服活性和可透过血脑屏障的 Smo 拮抗剂，IC50 值为 5.8 nM，Ki 值为 4.6 nM。PF-5274857 有潜力用于包括激活的 Hh 途径驱动的脑肿瘤和脑转移在内的多种肿瘤的研究。

PF-5274857

PF-5274857 Chemical Structure

CAS No. : 1373615-35-0

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 ￥1760 In-stock
5 mg ￥1600 In-stock
10 mg ￥2200 In-stock
50 mg ￥9000 In-stock
100 mg ￥15000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PF-5274857 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Anti-Aging Compound Library
  • Orally Active Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway[1].

IC50 & Target

IC50: 5.8 nM (Smo); Ki: 4.6 nM (Smo)[1]
体外研究
(In Vitro)

PF-5274857 completely inhibits Shh-induced Hh pathway activity with an IC50 of 2.7±1.4 nM measured by the transcriptional activity of Smo downstream gene Gli1 in MEF cells[1].
PF-5274857 shows less than 20% inhibition against a broad panel of protein kinases at 1 μM[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)

PF-5274857 (1-30 mg/kg; p.o. once daily for 6 days) shows robust antitumor efficacy and correlation between PK and PD in medulloblastoma allograft mice models[1].
PF-5274857 (10 mg/kg; i.h.) in the plasma is able to cross the blood-brain barrier in rats within 4 hours postdose[1].
PF-5274857 (10-100 mg/kg; p.o. once daily for 4 days) is able to target Smo in the brain leading to the downregulation of Hh pathway activity in the brain tumor[1].
PF-5274857 (30 mg/kg; p.o. once daily for 34 days) increases the survival rates of primary Ptch+/− p53−/− medulloblastoma mice[1].
PF-5274857 (5-30 mg/kg; p.o.) exhibits the apparent volume of distribution of 5.6±0.5 L/kg and the half-life (T1/2) of 1.7±0.1 hours[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 Model: Severe combined immunodeficient (SCID)-beige mice (6-8 weeks old) are genetically engineered[1]
Dosage: 0, 1, 5, 10, 30 mg/kg
Administration: P.o. once daily for 6 days
Result: Showed robust antitumor activity with an in vivo IC50 of 8.9±2.6 nM.
Animal Model: Severe combined immunodeficient (SCID)-beige mice (6-8 weeks old)[1]
Dosage: 0, 5, 10, 30 mg/kg (Pharmacokinetic Analysis)
Administration: A single p.o.
Result: The apparent volume of distribution of 5.6±0.5 L/kg; the half-life (T1/2) of 1.7±0.1 hours.

分子量

436.96

Formula

C20H25ClN4O3S
CAS 号

1373615-35-0
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 : 125 mg/mL (286.07 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2885 mL 11.4427 mL 22.8854 mL
5 mM 0.4577 mL 2.2885 mL 4.5771 mL
10 mM 0.2289 mL 1.1443 mL 2.2885 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 (4.76 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.76 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 (4.76 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.76 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 (4.76 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.76 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Rohner A, et al. Effective targeting of Hedgehog signaling in a medulloblastoma model with PF-5274857, a potent and selective Smoothened antagonist that penetrates the blood-brain barrier. Mol Cancer Ther. 2012, 11(1), 57-65.

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

ThrRS-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。

ThrRS-IN-1 

ThrRS-IN-1 (Compound 30d) 是一种 threonyl-tRNA synthetase (ThrRS) 抑制剂，对 Salmonella enterica ThrRS (SeThrRS) 的 IC50 值为 1.4 µM，Kd 值为 1.36 µM。 ThrRS-IN-1 同时靶向 ThrRS 的 tRNAThr 和 L-threonine 结合袋。ThrRS-IN-1 具有抗细菌 (antibacterial) 活性。

ThrRS-IN-1

ThrRS-IN-1 Chemical Structure

CAS No. : 2408626-64-0

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生物活性

ThrRS-IN-1 (Compound 30d) is a threonyl-tRNA synthetase (ThrRS) inhibitor with an IC50 of 1.4 µM and a Kd of 1.36 µM against Salmonella enterica ThrRS (SeThrRS). ThrRS-IN-1 simultaneously targets the tRNAThr and L-threonine binding pockets of ThrRS. ThrRS-IN-1 shows potent antibacterial activities[1].

IC50 & Target

IC50: 1.4 µM (SeThrRS)[1]
分子量

385.25

Formula

C16H18Cl2N4O3
CAS 号

2408626-64-0
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]. Junsong Guo, et al. Discovery of novel tRNA-amino acid dual-site inhibitors against threonyl-tRNA synthetase by fragment-based target hopping. Eur J Med Chem. 2020 Feb 1;187:111941.

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SKLB325

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。

SKLB325  纯度: 99.79%

SKLB325 是一种 JMJD6 抑制剂，其结合亲和力 (KD) 值为 0.755 μM，IC50 值为 0.7797 μM。SKLB325 在体内外对卵巢癌具有抗肿瘤作用。SKLB325 诱导细胞凋亡 (apoptosis)。SKLB325 在肾细胞癌 (RCC) 中表现出显着的抗肿瘤功效。

SKLB325

SKLB325 Chemical Structure

规格 价格 是否有货 数量
5 mg ￥3500 In-stock
10 mg ￥5200 In-stock
25 mg ￥9800 In-stock
50 mg ￥14200 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

SKLB325 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library

生物活性

SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755 μM, and the IC50 value of 0.7797 μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis[1]. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) [2].

体外研究
(In Vitro)

SKLB325 suppresses ovarian cancer growth through inhibition of proliferation and induction of apoptosis and cell death, and inhibiting angiogenesis may play a significant role in inhibiting tumor growth[1].
SKLB325 (0.25-16 μM; for 24-72 h) has significant inhibitory effects on the in vitro proliferation of ovarian cancer cells. Furthermore, the most effective concentration at which JMJD6 inhibited SKOV3 cell growth is 4 μM, and the optimal duration of action is 72 h[1].
SKLB325 upregulates the expression of p53 and its downstream effectors at both the mRNA and protein levels in vitro[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 Proliferation Assay[1]

Cell Line: SKOV3, ES2, A2780s and CP70 cells
Concentration: 0, 0.25, 0.5, 1, 2, 4, 8, and 16 μM
Incubation Time: 24 h, 48 h, and 72 h
Result: With increasing SKLB325 concentration, the inhibitory effect also increased, exhibiting a significant dose-response relationship. There was a significant difference between the drug group across different doses and the control group.

Western Blot Analysis[1]

Cell Line: SKOV3, ES2 and A2780s cells
Concentration: 4 μM
Incubation Time: 72 hours
Result: p53, p21, and PUMA protein levels were significantly upregulated in SKOV3, ES2 and A2780s cells.

体内研究
(In Vivo)

SKLB325 (10 mg/kg) has antitumor activities in an intraperitoneal xenograft model. SKLB325 significantly prolongs the survival of tumor-bearing mice without obvious side effects. SKLB325 treatment protocols were effective in suppressing SKOV3, ES2, CP70, and A2780s tumor growth in nude mice[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 Model: Female athymic BALB/c nude mice[1]
Dosage: 10 mg/kg
Administration: I.p. injections every three days for eight doses total
Result: The average weight of intraperitoneal tumor nodules was 1.56 ± 0.70, 1.04 ± 0.62, and 0.14 ± 0.11 g in the control, vehicle and SKLB325 groups, respectively. Tumor weight was significantly reduced by 91 and 86% in the SKLB325 groups compared to the control and vehicle groups, respectively.

分子量

244.25

Formula

C12H12N4O2
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 : 20.83 mg/mL (85.28 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 4.0942 mL 20.4708 mL 40.9417 mL
5 mM 0.8188 mL 4.0942 mL 8.1883 mL
10 mM 0.4094 mL 2.0471 mL 4.0942 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 (8.52 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.52 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% corn oil

    Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.52 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Heng Zheng, et al. Jumonji domain-containing 6 (JMJD6) identified as a potential therapeutic target in ovarian cancer. Signal Transduct Target Ther.2019 Jul 26;4:24.

    [2]. Chuanjie Zhang, et al. Epigenome screening highlights that JMJD6 confers an epigenetic vulnerability and mediates sunitinib sensitivity in renal cell carcinoma. Clin Transl Med. 2021 Feb;11(2):e328.

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BLM-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。

BLM-IN-1  纯度: 99.08%

BLM-IN-1 (compound 29) 是有效的、布鲁姆综合征蛋白 (BLM) 的抑制剂，对BLM的KD 值为1.81 μM，IC50 值为0.95 μM。可诱导DNA损伤反应，癌细胞的凋亡和增殖抑制。

BLM-IN-1

BLM-IN-1 Chemical Structure

CAS No. : 2056014-40-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5040 In-stock
5 mg ￥4500 In-stock
10 mg ￥7500 In-stock
50 mg ￥22500 In-stock
100 mg   询价  
200 mg   询价  

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BLM-IN-1 相关产品

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  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Targeted Diversity Library

生物活性

BLM-IN-1 (compound 29) is an effective Bloom syndrome protein (BLM) inhibitor, with a strong BLM binding KD of 1.81 μM and an IC50 of 0.95 μM for BLM. Induces DNA damage response, as well as apoptosis and proliferation arrest in cancer cells[1].

IC50 & Target

IC50: 1.95 μM (BLM)[1].
分子量

462.60

Formula

C28H35FN4O
CAS 号

2056014-40-3
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 : 8.33 mg/mL (18.01 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1617 mL 10.8085 mL 21.6169 mL
5 mM 0.4323 mL 2.1617 mL 4.3234 mL
10 mM 0.2162 mL 1.0808 mL 2.1617 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。
参考文献

  • [1]. Yin QK, et al. Discovery of Isaindigotone Derivatives as Novel Bloom’s Syndrome Protein (BLM) Helicase Inhibitors That Disrupt the BLM/DNA Interactions and Regulate the Homologous Recombination Repair. J Med Chem. 2019 Mar 28;62(6):3147-3162.

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Borussertib

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。

Borussertib  纯度: 98.59%

Borussertib 是蛋白激酶 Akt 的首创的、共价变构抑制剂，其对 Aktwt 的IC50 值为 0.8 nM，Ki 值为 2.2 nM。

Borussertib

Borussertib Chemical Structure

CAS No. : 1800070-77-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4594 In-stock
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
25 mg ￥9900 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Borussertib 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
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  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Differentiation Inducing Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Anti-Obesity Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt[1].

IC50 & Target[1]

Aktwt

0.8 nM (IC50)

Aktwt

2.2 nM (Ki)

体外研究
(In Vitro)

Borussertib exhibits excellent cellular activity in the nanomolar range with superior profile against clinical candidate Akt inhibitors as well as the cytostatic drug doxorubicin. The EC50 values are 191±90 nM, 48±15 nM, 5±1 nM, 277±90 nM, 373±54 nM, 7770±641 nM in AN3CA (endometrium), T47D (breast), ZR-75-1 (breast), MCF-7 (breast), BT-474 (breast) and KU-19-19 (bladder) cell lines, 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

596.68

Formula

C36H32N6O3
CAS 号

1800070-77-2
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 : 25 mg/mL (41.90 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6759 mL 8.3797 mL 16.7594 mL
5 mM 0.3352 mL 1.6759 mL 3.3519 mL
10 mM 0.1676 mL 0.8380 mL 1.6759 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 (3.49 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.49 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% corn oil

    Solubility: ≥ 2.08 mg/mL (3.49 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.49 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Niklas Uhlenbrock, et al. Structural and chemical insights into the covalentallosteric inhibition of the protein kinase Akt. Chem Sci., 2019, 10, 3573.

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

BLU9931

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。

BLU9931  纯度: 99.95%

BLU9931 是一种有效的，高度选择性的，不可逆的成纤维细胞生长因子受体 4 (FGFR4) 抑制剂，其 IC50 值为 3 nM，Kd 值为 6 nM。BLU9931 具有显着的抗肿瘤活性。

BLU9931

BLU9931 Chemical Structure

CAS No. : 1538604-68-0

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 ￥1045 In-stock
5 mg ￥950 In-stock
10 mg ￥1500 In-stock
50 mg ￥3900 In-stock
100 mg ￥6600 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

BLU9931 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Reprogramming Compound Library
  • Chemical Probe Library
  • Anti-Lung Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library

生物活性

BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 3 nM and a Kd of 6 nM. BLU9931 has significant antitumor activity[1].

IC50 & Target

FGFR1

591 nM (IC50)

FGFR2

493 nM (IC50)

FGFR3

150 nM (IC50)

FGFR4

3 nM (IC50)

体外研究
(In Vitro)

BLU9931 inhibits proliferation of HCC cell lines that express an intact FGFR4 signaling complex, with EC50s of 0.07 μM, 0.11 μM and 0.02 μM for Hep 3B, HuH7 and JHH7 cells, respectively[1].
BLU9931 (0.3-300 nM; 1 hour; MDA-MB-453 and Hep 3B cells) treatment demonstrates potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 cells. BLU9931 shows dose-dependent inhibition of the signaling cascade downstream of FGFR4. BLU9931 exhibits potent inhibition of phosphorylation of the FGFR4 pathway components in Hep 3B cells. BLU9931 treatment leads to induction of caspase-3/7 activity, indicative of induction of apoptosis that results in inhibition of signaling downstream of FGFR4[1].
BLU9931 (100 nM; 0 -24 hours; Hep 3B cells) treatment increases CYP7A1 mRNA expression and the expression of the proliferative marker EGR1 is inhibited[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.

Western Blot Analysis[1]

Cell Line: MDA-MB-453 and Hep 3B cells
Concentration: 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
Incubation Time: 1 hour
Result: Demonstrated potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 and Hep 3B cells.

RT-PCR[1]

Cell Line: Hep 3B cells
Concentration: 100 nM
Incubation Time: 0 hour, 4 hours, 8 hour, 24 hours
Result: Increased CYP7A1 mRNA expression. And the expression of the proliferative marker EGR1 was inhibited.

体内研究
(In Vivo)

BLU9931 (10-100 mg/kg; oral administration; twice every day; for 21 days; mice) treatment demonstrates antitumor activity in HCC xenograft models[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 Model: Mice injected with Hep 3B cells[1]
Dosage: 10 mg/kg, 30 mg/kg or 100 mg/kg
Administration: Oral administration; twice every day; for 21 days
Result: Resulted in dose-dependent growth inhibition of Hep 3B tumors. Prevented weight loss in a dose-dependent manner.

分子量

509.38

Formula

C26H22Cl2N4O3
CAS 号

1538604-68-0
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 : 125 mg/mL (245.40 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9632 mL 9.8159 mL 19.6317 mL
5 mM 0.3926 mL 1.9632 mL 3.9263 mL
10 mM 0.1963 mL 0.9816 mL 1.9632 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 (4.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.08 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 (4.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.08 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 (4.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.08 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Hagel M, et al. First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov. 2015 Apr;5(4):424-37.

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

AS-605240

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。

AS-605240  纯度: 99.17%

AS-605240 是一种口服有效的特异性 PI3Kγ 抑制剂，IC50 值为 8 nM，Ki 值为 7.8 nM。

AS-605240

AS-605240 Chemical Structure

CAS No. : 648450-29-7

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 ￥729 In-stock
10 mg ￥663 In-stock
50 mg ￥2400 In-stock
100 mg ￥3938 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AS-605240 相关产品

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生物活性

AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.

IC50 & Target

PI3Kα

60 nM (IC50)

PI3Kβ

270 nM (IC50)

PI3Kδ

300 nM (IC50)

PI3Kγ

8 nM (IC50)

PI3Kγ

7.8 nM (Ki)

Autophagy

 

体外研究
(In Vitro)

AS-605240 is an isoform-selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18- and 7.5-fold selectivity over PI3Kα, respectively. AS-605240 shows an inhibitory effect on C5a-mediated PKB phosphorylation in RAW264 mouse macrophages with an IC50 of 0.09 μM. AS-605240 blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1. AS-605240 inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α and β in a concentration-dependent manner. AS605240 suppresses in a dose-dependent manner the proliferation of BDC2.5 CD4+ T cells[2].

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)

AS-605240 (30 mg/kg BW, per os, every 12 h) markedly decreases FoxM1 expression in mouse lungs and fails to restore vascular integrity[1]. AS-605240 reduces RANTES-induced peritoneal neutrophil recruitment, with ED50 of 9.1 mg/kg. In the CCL5 model, AS-605240 shows an ED50 value of 10 mg/kg, in correlation with the percentage of reduction of neutrophil recruitment observed in Pik3cg-/- mice. AS-605240 (50 mg/kg, p.o.) substantially reduces clinical and histological signs of joint inflammation to a similar extent to that of Pik3cg-/- mice[2]. AS605240 (30 mg/kg, i.p.) suppresses intracellular PAkt in splenocytes of NOD mice and delays diabetes onset. AS605240 also prevents autoimmune diabetes in prediabetic NOD mice, and suppresses autoreactive T cells while increasing Tregs in NOD mice. AS605240 (30 mg/kg, i.p.) reverses hyperglycemia in newly hyperglycemic NOD mice, reverses hyperglycemia in early diabetic NOD mice through Tregs and suppresses T-cell infiltration in pancreatic islets while increasing Tregs[3]. AS605240 (25, 50 mg/kg) markedly reduces total cell count and numbers of macrophages, neutrophils and lymphocytes in rats. AS605240 significantly reduces the levels of TNF-α and IL-1β in BALF to 132.7±11.2 pg/mL and 49.2±11.3 pg/mL in 25 mg/kg AS605240 + BLM group and 131.3±10.7 and 49.6±8.8 pg/mL in 50 mg/kg AS605240 + BLM group, respectively. AS605240 inhibits prefibrotic cytokines production in bleomycin-induced pulmonary fibrosis. AS605240 inhibits phosphorylation of Akt of inflammatory cells in bleomycin-induced pulmonary fibrosis model[4].

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

257.27

Formula

C12H7N3O2S
CAS 号

648450-29-7
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 : 5.8 mg/mL (22.54 mM; Need warming)

H2O : 2.78 mg/mL (10.81 mM; ultrasonic and warming and adjust pH to 10 with NaOH 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 3.8870 mL 19.4348 mL 38.8697 mL
5 mM 0.7774 mL 3.8870 mL 7.7739 mL
10 mM 0.3887 mL 1.9435 mL 3.8870 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： 0.5% CMC-Na  0.5% Tween-80

    Solubility: 6.25 mg/mL (24.29 mM); Suspened solution; Need ultrasonic

  • 2.

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

    Solubility: 2.5 mg/mL (9.72 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (9.72 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 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

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (9.72 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.72 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 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Huang X, et al. Endothelial p110γPI3K Mediates Endothelial Regeneration and Vascular Repair After Inflammatory Vascular Injury. Circulation. 2016 Mar 15;133(11):1093-103.

    [2]. Camps M, et al. Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005 Sep;11(9):936-43.

    [3]. Azzi J, et al. The novel therapeutic effect of phosphoinositide 3-kinase-γ inhibitor AS605240 in autoimmune diabetes. Diabetes. 2012 Jun;61(6):1509-18. Epub 2012 Mar 8.

    [4]. Wei X, et al. A phosphoinositide 3-kinase-gamma inhibitor, AS605240 prevents bleomycin-induced pulmonary fibrosis in rats. Biochem Biophys Res Commun. 2010 Jun 25;397(2):311-7. Epub 2010 May 26.
Kinase Assay
[2]

Human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl2, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na3VO4, 0.1% Na Cholate and 15 M ATP/100 nCi γ[33P]ATP, final concentrations) and lipid vesicles containing 18 M PtdIns and 250 M of PtdSer (final concentrations), in the presence of inhibitors or DMSO. Kinase reaction is stopped by adding 250 g of Neomycin-coated Scintillation Proximity Assay (SPA) bead and proceeded.

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
[3]

A total of 5×105 BDC2.5 splenocytes and 50 μg/mL BDC2.5-peptide are incubated in vitro in a 96-well round-bottom plate for 48 h. Then the cultures are pulsed with 1 μCi of tritiated thymidine [3H] to determine cell proliferation.

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
[4]

In this study, rats are bred for one week to affirm body weight and then randomLy divided into four experimental groups: (a) control group (rats are given vehicle only); (b) BLM group (rats are induced with BLM); (c) BLM + 25 mg/kg AS605240 group (rats are induced with BLM and then administrated with 25 mg/kg AS605240); (d) BLM + 50 mg/kg AS605240 group (the same protocol as the former group except a different dose of 50 mg/kg AS605240). In addition, five rats are given 50 mg/kg AS605240 only to detect whether AS605240 has any side effect simultaneously as the previous four groups. Rats in (c), (d) and AS605240-given-only group are administered orally 25, 50 and 50 mg/kg AS605240 by gavage while rats in control group and BLM group are given only equivalent saline at day-1 (the day rats are given BLM is marked as day-0). The same dosage is maintained once everyday for 28 days.

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]. Huang X, et al. Endothelial p110γPI3K Mediates Endothelial Regeneration and Vascular Repair After Inflammatory Vascular Injury. Circulation. 2016 Mar 15;133(11):1093-103.

    [2]. Camps M, et al. Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005 Sep;11(9):936-43.

    [3]. Azzi J, et al. The novel therapeutic effect of phosphoinositide 3-kinase-γ inhibitor AS605240 in autoimmune diabetes. Diabetes. 2012 Jun;61(6):1509-18. Epub 2012 Mar 8.

    [4]. Wei X, et al. A phosphoinositide 3-kinase-gamma inhibitor, AS605240 prevents bleomycin-induced pulmonary fibrosis in rats. Biochem Biophys Res Commun. 2010 Jun 25;397(2):311-7. Epub 2010 May 26.

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