标签归档：pki

PKI 14-22 amide,myristoylated

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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。

PKI 14-22 amide,myristoylated  纯度: 99.65%

PKI 14-22 amide,myristoylated 是一种有效的 cAMP 依赖性 PKA 抑制剂。PKI 14-22 amide,myristoylated 可降低 IgG 介导的吞噬反应，也可抑制中性粒细胞粘附。

PKI 14-22 amide,myristoylated

PKI 14-22 amide,myristoylated Chemical Structure

CAS No. : 201422-03-9

规格 价格 是否有货 数量
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5 mg ￥4500 In-stock
10 mg   询价  
50 mg   询价  

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PKI 14-22 amide,myristoylated 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Peptide Library

生物活性

PKI 14-22 amide,myristoylated is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion[1].

分子量

1209.49

Formula

C53H100N20O12
CAS 号

201422-03-9
Sequence Shortening

Myristoyl-GRTGRRNAI-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O

Peptide Solubility and Storage Guidelines:

1.  Calculate the length of the peptide.

2.  Calculate the overall charge of the entire peptide according to the following table:

  Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.  Recommended solution:

Overall charge of peptide Details
Negative (<0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, add NH4OH (<50 μL).
3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>0) 1.  Try to dissolve the peptide in water first.
2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. L Ydrenius, et al. Activation of cAMP-dependent protein kinase is necessary for actin rearrangements in human neutrophils during phagocytosis. J Leukoc Biol. 2000 Apr;67(4):520-8.

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PKI-166

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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。

PKI-166  纯度: 98.78%

PKI-166 是一种高效、选择性的，有口服生物活性的 EGFR 酪氨酸激酶抑制剂，IC50 值为 0.7 nM。

PKI-166

PKI-166 Chemical Structure

CAS No. : 187724-61-4

规格 价格 是否有货 数量
5 mg ￥5600 In-stock
10 mg ￥9500 询价
50 mg   询价  
100 mg   询价  

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PKI-166 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].

IC50 & Target

IC50: 0.7 nM (EGFR tyrosine kinase)[1]
体外研究
(In Vitro)

Pretreatment with PKI-166 (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1].
PKI-166 (0.03μ M; 6 days) enhanced the cytotoxicity mediated by gemcitabine[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: L3.6pl cells
Concentration: 0.01 μM, 0.05 μM, 0.5 μM
Incubation Time: 1 hour
Result: Inhibited EGFR autophosphorylation in a dose-dependent manner.

Cell Cytotoxicity Assay[1]

Cell Line: L3.6pl cells
Concentration: 0.03 μM
Incubation Time: 6 days
Result: Enhanced the cytotoxicity mediated by gemcitabine.

体内研究
(In Vivo)

PKI-166 (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) inhibits of pancreatic cancer growth[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: Male athymic nude mice with L3.6pl cells xenograft (8–12 weeks)[1]
Dosage: 100 mg/kg
Administration: Oral administration; daily; from day 7 to day 35 after xenograft
Result: Significantly decreased median tumor volume.

分子量

330.38

Formula

C20H18N4O
CAS 号

187724-61-4
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
参考文献

  • [1]. Bruns CJ, et al. Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 2000 Jun 1;60(11):2926-35.

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

PKI-166 hydrochloride

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。

PKI-166 hydrochloride 

PKI-166 hydrochloride 是一种高效、选择性的，具有口服生物活性的 EGFR 酪氨酸激酶抑制剂，IC50 值为 0.7 nM。

PKI-166 hydrochloride

PKI-166 hydrochloride Chemical Structure

CAS No. : 2230253-82-2

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

* Please select Quantity before adding items.

PKI-166 hydrochloride 的其他形式现货产品:

PKI-166

生物活性

PKI-166 hydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].

IC50 & Target

IC50: 0.7 nM (EGFR tyrosine kinase)[1]
体外研究
(In Vitro)

PKI-166 hydrochloride (0-0.5 μM; 1 hour; pretreatment) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1].
PKI-166 hydrochloride (0.03 μM; 6 days) enhances the cytotoxicity mediated by gemcitabine[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: L3.6pl cells
Concentration: 0.01 μM, 0.05 μM, 0.5 μM
Incubation Time: 1 hour
Result: Inhibited EGFR autophosphorylation in a dose-dependent manner.

Cell Cytotoxicity Assay[1]

Cell Line: L3.6pl cells
Concentration: 0.03 μM
Incubation Time: 6 days
Result: Enhanced the cytotoxicity mediated by gemcitabine.

体内研究
(In Vivo)

PKI-166 hydrochloride (100 mg/kg; p.o.; daily; for 29 days) inhibits of pancreatic cancer growth[1].

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

Animal Model: Male athymic nude mice with L3.6pl cells xenograft (8-12 weeks)[1]
Dosage: 100 mg/kg
Administration: Oral administration; daily; for 29 days
Result: Significantly decreased median tumor volume.

分子量

366.84

Formula

C20H19ClN4O
CAS 号

2230253-82-2
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]. Bruns CJ, et al. Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 2000 Jun 1;60(11):2926-35.

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

PKI-166 hydrochloride

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。

PKI-166 hydrochloride 

PKI-166 hydrochloride 是一种高效、选择性的，具有口服生物活性的 EGFR 酪氨酸激酶抑制剂，IC50 值为 0.7 nM。

PKI-166 hydrochloride

PKI-166 hydrochloride Chemical Structure

CAS No. : 2230253-82-2

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

* Please select Quantity before adding items.

PKI-166 hydrochloride 的其他形式现货产品:

PKI-166

生物活性

PKI-166 hydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].

IC50 & Target

IC50: 0.7 nM (EGFR tyrosine kinase)[1]
体外研究
(In Vitro)

PKI-166 hydrochloride (0-0.5 μM; 1 hour; pretreatment) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1].
PKI-166 hydrochloride (0.03 μM; 6 days) enhances the cytotoxicity mediated by gemcitabine[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: L3.6pl cells
Concentration: 0.01 μM, 0.05 μM, 0.5 μM
Incubation Time: 1 hour
Result: Inhibited EGFR autophosphorylation in a dose-dependent manner.

Cell Cytotoxicity Assay[1]

Cell Line: L3.6pl cells
Concentration: 0.03 μM
Incubation Time: 6 days
Result: Enhanced the cytotoxicity mediated by gemcitabine.

体内研究
(In Vivo)

PKI-166 hydrochloride (100 mg/kg; p.o.; daily; for 29 days) inhibits of pancreatic cancer growth[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: Male athymic nude mice with L3.6pl cells xenograft (8-12 weeks)[1]
Dosage: 100 mg/kg
Administration: Oral administration; daily; for 29 days
Result: Significantly decreased median tumor volume.

分子量

366.84

Formula

C20H19ClN4O
CAS 号

2230253-82-2
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]. Bruns CJ, et al. Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 2000 Jun 1;60(11):2926-35.

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

PKI-166 hydrochloride

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。

PKI-166 hydrochloride 

PKI-166 hydrochloride 是一种高效、选择性的，具有口服生物活性的 EGFR 酪氨酸激酶抑制剂，IC50 值为 0.7 nM。

PKI-166 hydrochloride

PKI-166 hydrochloride Chemical Structure

CAS No. : 2230253-82-2

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

* Please select Quantity before adding items.

PKI-166 hydrochloride 的其他形式现货产品:

PKI-166

生物活性

PKI-166 hydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].

IC50 & Target

IC50: 0.7 nM (EGFR tyrosine kinase)[1]
体外研究
(In Vitro)

PKI-166 hydrochloride (0-0.5 μM; 1 hour; pretreatment) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1].
PKI-166 hydrochloride (0.03 μM; 6 days) enhances the cytotoxicity mediated by gemcitabine[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: L3.6pl cells
Concentration: 0.01 μM, 0.05 μM, 0.5 μM
Incubation Time: 1 hour
Result: Inhibited EGFR autophosphorylation in a dose-dependent manner.

Cell Cytotoxicity Assay[1]

Cell Line: L3.6pl cells
Concentration: 0.03 μM
Incubation Time: 6 days
Result: Enhanced the cytotoxicity mediated by gemcitabine.

体内研究
(In Vivo)

PKI-166 hydrochloride (100 mg/kg; p.o.; daily; for 29 days) inhibits of pancreatic cancer growth[1].

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

Animal Model: Male athymic nude mice with L3.6pl cells xenograft (8-12 weeks)[1]
Dosage: 100 mg/kg
Administration: Oral administration; daily; for 29 days
Result: Significantly decreased median tumor volume.

分子量

366.84

Formula

C20H19ClN4O
CAS 号

2230253-82-2
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]. Bruns CJ, et al. Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 2000 Jun 1;60(11):2926-35.

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

多肽定制PKI-tide 编码 [126370-52-3]

发表于由

上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 PKI-tide
编码 [126370-52-3]
别名 PKI-tide
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） IAAGRTGRRQAIHDILVAA
序列（三字母缩写） Ile-Ala-Ala-Gly-Arg-Thr-Gly-Arg-Arg-Gln-Ala-Ile-His-Asp-Ile-Leu-Val-Ala-Ala
基本描述
溶解度
分子量 1989.31
化学式 C85H149N31O24
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents PKI-tide 编码 [126370-52-3]
Figures PKI-tide 编码 [126370-52-3]
Reference
C端
N端
化学桥

多肽定制PKI-tide 编码 [126370-52-3]

发表于由

上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 PKI-tide
编码 [126370-52-3]
别名 PKI-tide
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） IAAGRTGRRQAIHDILVAA-OH
序列（三字母缩写） Ile-Ala-Ala-Gly-Arg-Thr-Gly-Arg-Arg-Gln-Ala-Ile-His-Asp-Ile-Leu-Val-Ala-Ala
基本描述
溶解度
分子量 0
化学式
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents PKI-tide 编码 [126370-52-3]
Figures PKI-tide 编码 [126370-52-3]
Reference
C端
N端
化学桥

PKI-402

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。

PKI-402  纯度: 99.79%

PKI-402 是一种有效的 PI3K 和 mTOR 抑制剂，抑制 PI3Kα, mTOR, PI3Kβ, PI3Kδ 和 PI3Kγ，IC50 分别为 2, 3, 7, 14 和 16 nM。

PKI-402

PKI-402 Chemical Structure

CAS No. : 1173204-81-3

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥1534 In-stock
10 mg ￥2558 In-stock
50 mg ￥7161 In-stock
100 mg ￥12741 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PKI-402 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • 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
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton 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
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).

IC50 & Target[1]

PI3Kα

2 nM (IC50)

PI3Kα-H1047R

3 nM (IC50)

PI3Kα-E545K

3 nM (IC50)

PI3Kβ

7 nM (IC50)

PI3Kδ

14 nM (IC50)

PI3Kγ

16 nM (IC50)

mTOR

3 nM (IC50)

体外研究
(In Vitro)

PKI-402 is an equipotent inhibitor of class I PI3K, including the E545K and H1047R PI3K-α mutants (IC50=2, 3 and 3 nM for PI3Kα, PI3Kα-H1047R and PI3Kα-E545K, respectively). PKI-402 causes in vitro growth inhibition of human tumor cell lines derived from a diverse set of human tumor tissues, including breast, brain (glioma), pancreas, and non-small cell lung cancer (NSCLC) tissues. PKI-402 inhibits MDA-MB-361 [breast: Her2+ and PIK3CA mutant (E545K)], with an IC50 of 6 nM. PKI-402 inhibits HCT116 (K-Ras and PIK3CA mutant) with an IC50 of 33 nM[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)

PKI-402 displays antitumor activity (i.v. route) in breast [MDA-MB-361: Her2+ and PIK3CA (E545K)], glioma (U87MG and PTEN), and NSCLC (A549; K-Ras and STK11) xenograft models. PKI-402 causes regression in the MDA-MB-361 xenograft model. PKI-402 effect is most pronounced at 100 mg/kg (daily for 5 days, one round), which reduces initial tumor volume and prevents tumor re-growth for 70 days. In MDA-MB-361 tumor tissue, PKI-402 at 100 mg/kg (single dose) fully suppresses p-Akt at both the T308 and the S473 sites at 8 hours and induces cleaved PARP. At 24 hours, p-Akt suppression is still evident, as is cleaved PARP[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

570.65

Formula

C29H34N10O3
CAS 号

1173204-81-3
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 : 5 mg/mL (8.76 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7524 mL 8.7619 mL 17.5239 mL
5 mM 0.3505 mL 1.7524 mL 3.5048 mL
10 mM — — —

*

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]. Mallon R et al. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol Cancer Ther. 2010 Apr;9(4):976-84.
Kinase Assay
[1]

Enzyme assays are done in fluorescent polarization (FP) format. Human class I PI3Ks and PI3K-α mutants (E545K and H1047R) are produced in Sf9. GST-GRP1 (murine) is produced in Escherichia coli and isolated by GST-Sepharose. Assay buffers are reaction buffer [20 mM HEPES (pH 7.1), 2 mM MgCl2, 0.05% CHAPS, and 0.01% β-mercaptoethanol] and stop/detection buffer [100 mM HEPES (pH 7.5), 4 mM EDTA, 0.05% CHAPS]. FP reaction is run for 30 min at room temperature in 20 μL of reaction buffer containing 20 μM phosphatidylinositol 4,5-bisphosphate (PIP2), 25 μM ATP, and <4% DMSO (compound solvent). FP reaction is stopped with 20 μL of stop/detection buffer (10 nM probe and 40 nM GST-GRP), and after 2 h, data are collected. Selectivity of PKI-402 is evaluated in the 236 human kinase panel at [ATP]=Km for each enzyme[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]

MDA-MB-361, MDA-MB-468, T47D, MCF7, BT474, HT29, HCT116, DLD1, U87MG, H157, NCI-H460, A549, NCI-H1975, NCI-H1650, NCI-H2170, KB, 786-0, A498, MIA-PaCa-2, and PC3 cell lines are propagated at 37°C in 5% CO2 incubators in supplier-recommended growth medium. Cell growth inhibition is determined using the CellTiter 96 AQueous proliferation assay. Data are collected after 72 h using a Wallac Victor2 V 1420 multilabel HTS counter. FOXO-GFP translocation in U2OS cells is quantified after 60-min PKI-402 exposure using a Cellomics ArrayScan VTI Reader[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]
PKI-402 or vehicle is administered by i.v. route. Nude mice bearing MDA-MB-361 tumors are used. Tumor weight is calculated. Pharmacodynamic (biomarker) measurements are done on tumor-bearing female nude mice administered PKI-402. Tumor or normal tissue samples are collected from euthanized animals, homogenized, washed twice with cold (4°C) PBS, and then treated with cell lysis buffer[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.
参考文献

  • [1]. Mallon R et al. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol Cancer Ther. 2010 Apr;9(4):976-84.

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Gedatolisib(Synonyms: PKI-587; PF-05212384)

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。

Gedatolisib (Synonyms: PKI-587; PF-05212384) 纯度: 99.68%

Gedatolisib (PKI-587) 是一种高效的双重 PI3Kα，PI3Kγ 和 mTOR 抑制剂, IC50 分别为 0.4 nM，5.4 nM 和 1.6 nM。Gedatolisib 在 mTOR 复合物 mTORC1 和 mTORC2 中同样有效。

Gedatolisib(Synonyms: PKI-587; PF-05212384)

Gedatolisib Chemical Structure

CAS No. : 1197160-78-3

规格 价格 是否有货 数量
5 mg ￥990 In-stock
10 mg ￥1700 In-stock
50 mg ￥4900 In-stock
100 mg ￥8500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Gedatolisib 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively[1]. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2[2].

IC50 & Target[1][3]

PI3Kα

0.4 nM (IC50)

PI3Kα-H1047R

0.6 nM (IC50)

PI3Kα-E545K

0.6 nM (IC50)

PI3Kγ

5.4 nM (IC50)

PI3Kβ

6 nM (IC50)

PI3Kδ

6 nM (IC50)

mTOR

1.6 nM (IC50)

mTORC1

 

mTORC2

 

体外研究
(In Vitro)

Gedatolisib (PKI-587) shows good potency in cell growth inhibition assays using MDA-361 and PC3-MM2 cell lines with IC50s of 4.0 and 13.1 nM, respectively[1].
Gedatolisib shows potent suppression of phosphorylation of PI3K/mTOR signaling pathway proteins in MDA-361 tumor cells. Gedatolisib (0.03-3 μM; 4 hours) prevents the phosphorylation of Akt at Thr 308 and induces cleaved PARP at 30 nM[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-361 tumor cells
Concentration: 0.03, 0.1, 0.3, 1, and 3 μM
Incubation Time: 4 hours
Result: Prevented the phosphorylation of Akt (pAkt) at threonine 308 (T308; IC50=8 nM).

体内研究
(In Vivo)

Gedatolisib (PKI-587; administered i.v. at 20 mg/kg on days 1, 5, 9) exhibits potent antitumor efficacy against MDA-361 tumors in mice[1].
Gedatolisib exhibits terminal elimination half-life (T1/2 14.4 h) due to high plasma clearance (7 mL/min/kg) combined with large volumes of distribution (7.2 L/kg respectively) following i.v. administration (25 mg/kg) female 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 nude mice bearing MDA-361 xenograft model[1].
Dosage: 20 mg/kg
Administration: Administered i.v. at 20 mg/kg on an intermittent regimen (days 1, 5, 9).
Result: Caused regression of large staged (~900 mm3) tumors.
The minimum efficacious dose (MED) was determined to be 3 mg/kg against MDA-361 tumors and maximum tolerated single dose (MTD) was determined to be 30 mg/kg.

分子量

615.73

Formula

C32H41N9O4
CAS 号

1197160-78-3
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.
溶解性数据
In Vitro: 

DMSO : 4 mg/mL (6.50 mM; Need warming)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6241 mL 8.1204 mL 16.2409 mL
5 mM 0.3248 mL 1.6241 mL 3.2482 mL
10 mM — — —

参考文献

  • [1]. Venkatesan AM, et al. Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5′-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J Med Chem. 2010, 53(6), 2636-2645.

    [2]. Freitag H, et al. Inhibition of mTOR’s Catalytic Site by PKI-587 Is a Promising Therapeutic Option for Gastroenteropancreatic Neuroendocrine Tumor Disease. Neuroendocrinology. 2017;105(1):90-104.

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PKI-179

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。

PKI-179  纯度: ≥98.0%

PKI-179 是一种有效的和具有口服活性的双重 PI3K/mTOR 抑制剂，对 PI3K-α，PI3K-β，PI3K-γ，PI3K-δ 和 mTOR 的 IC50 值分别为 8 nM，24 nM，74 nM，77 nM 和 0.42 nM。PKI-179 还表现出对 E545K 和 H1047R 的活性，IC50 值分别为 14 nM 和 11 nM。PKI-179 在体内显示出抗肿瘤活性。

PKI-179

PKI-179 Chemical Structure

CAS No. : 1197160-28-3

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 ￥2690 In-stock
5 mg ￥2500 In-stock
10 mg ￥4000 In-stock
25 mg ￥8000 In-stock
50 mg ￥12800 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

PKI-179 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton 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
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo[1][2].

IC50 & Target[1]

PI3Kα

8 nM (IC50)

PI3Kβ

24 nM (IC50)

PI3Kγ

74 nM (IC50)

PI3Kδ

77 nM (IC50)

mTOR

0.42 nM (IC50)

E545K

14 nM (IC50)

H1047R

11 nM (IC50)

体外研究
(In Vitro)

PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].
PKI-179 shows inhibitory activity against a panel of 361 other kinases, hERG and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but does have activity for CYP2C8 (IC50=3 μM)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

PKI-179 (5-50 mg/kg; p.o. once daily for 40 days) inhibits the tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors[1].
PKI-179 (50 mg/kg; p.o.) results in good inhibition of PI3K signaling in nude mice bearing MDA361 tumor xenografts[1].
PKI-179 exhibits good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min) [1].

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

Animal Model: Nude mice bearing MDA-361 human breast cancer tumors[1]
Dosage: 5, 10, 25, 50 mg/kg
Administration: I.p. every 3 days for 4 weeks
Result: Exhibited pronounced tumor growth arrest when dosed above 10 mg/kg.
No significant weight loss of tested animals was observed for all different dosages.

Clinical Trial

分子量

488.54

Formula

C25H28N8O3
CAS 号

1197160-28-3
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 (204.69 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0469 mL 10.2346 mL 20.4692 mL
5 mM 0.4094 mL 2.0469 mL 4.0938 mL
10 mM 0.2047 mL 1.0235 mL 2.0469 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: ≥ 2.5 mg/mL (5.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.12 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
  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

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

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Venkatesan AM, et, al. PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5869-73.

    [2]. Rehan M. A structural insight into the inhibitory mechanism of an orally active PI3K/mTOR dual inhibitor, PKI-179 using computational approaches. J Mol Graph Model. 2015 Nov;62:226-234.

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

PKI-179 hydrochloride

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。

PKI-179 hydrochloride  纯度: 98.11%

PKI-179 hydrochloride 是一种有效的和具有口服活性的双重 PI3K/mTOR 抑制剂，对 PI3K-α，PI3K-β，PI3K-γ，PI3K-δ 和 mTOR 的 IC50 值分别为 8 nM，24 nM，74 nM，77 nM 和 0.42 nM。PKI-179 hydrochloride 还表现出对 E545K 和 H1047R 的活性，IC50 值分别为 14 nM 和 11 nM。PKI-179 hydrochloride 在体内显示出抗肿瘤活性。

PKI-179 hydrochloride

PKI-179 hydrochloride Chemical Structure

CAS No. : 1463510-35-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2890 In-stock
5 mg ￥2500 In-stock
10 mg ￥4000 In-stock
25 mg ￥8000 In-stock
50 mg ￥12800 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

PKI-179 hydrochloride 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton 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
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo[1][2].

IC50 & Target[1]

mTOR

0.42 nM (IC50)

PI3Kα

8 nM (IC50)

PI3Kβ

24 nM (IC50)

PI3Kγ

74 nM (IC50)

PI3Kδ

77 nM (IC50)

E545K

14 nM (IC50)

H1047R

77 nM (IC50)

体外研究
(In Vitro)

PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].
PKI-179 shows inhibitory activity against a panel of 361 other kinases, hERG and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but does have activity for CYP2C8 (IC50=3 μM)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

PKI-179 (5-50 mg/kg; p.o. once daily for 40 days) inhibits the tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors[1].
PKI-179 (50 mg/kg; p.o.) results in good inhibition of PI3K signaling in nude mice bearing MDA361 tumor xenografts[1].
PKI-179 exhibits good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min) [1].

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

Animal Model: Nude mice bearing MDA-361 human breast cancer tumors[1]
Dosage: 5, 10, 25, 50 mg/kg
Administration: I.p. every 3 days for 4 weeks
Result: Exhibited pronounced tumor growth arrest when dosed above 10 mg/kg.
No significant weight loss of tested animals was observed for all different dosages.

Clinical Trial

分子量

525.00

Formula

C25H29ClN8O3
CAS 号

1463510-35-1
运输条件

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (63.49 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 1.9048 mL 9.5238 mL 19.0476 mL
5 mM 0.3810 mL 1.9048 mL 3.8095 mL
10 mM 0.1905 mL 0.9524 mL 1.9048 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 (sealed storage, away from moisture)。-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: ≥ 1.25 mg/mL (2.38 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.38 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 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: ≥ 1.25 mg/mL (2.38 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.38 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 12.5 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]. Venkatesan AM, et, al. PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5869-73.

    [2]. Rehan M. A structural insight into the inhibitory mechanism of an orally active PI3K/mTOR dual inhibitor, PKI-179 using computational approaches. J Mol Graph Model. 2015 Nov;62:226-234.

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

PKI 14-22 amide,myristoylated TFA

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。

PKI 14-22 amide,myristoylated TFA  纯度: 99.86%

PKI 14-22 amide,myristoylated TFA 是一种有效的 cAMP 依赖性 PKA 抑制剂。PKI 14-22 amide,myristoylated TFA 可降低 IgG 介导的吞噬反应，也可抑制中性粒细胞粘附。

PKI 14-22 amide,myristoylated TFA

PKI 14-22 amide,myristoylated TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ￥1600 In-stock
10 mg ￥2700 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

PKI 14-22 amide,myristoylated TFA 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

PKI 14-22 amide,myristoylated TFA is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated TFA reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion[1].

分子量

1323.51

Formula

C55H101F3N20O14
Sequence Shortening

Myristoyl-GRTGRRNAI-NH2
运输条件

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

Protect from light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

H2O : 1.85 mg/mL (1.40 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7556 mL 3.7778 mL 7.5557 mL
5 mM — — —
10 mM — — —

*

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 (protect from light)。-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]. L Ydrenius, et al. Activation of cAMP-dependent protein kinase is necessary for actin rearrangements in human neutrophils during phagocytosis. J Leukoc Biol. 2000 Apr;67(4):520-8.

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