PI3K/mTOR Inhibitor-6

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。

PI3K/mTOR Inhibitor-6 

PI3K/mTOR Inhibitor-6 (Compound 19c) 是一种有效的 PI3K/mTOR 双重抑制剂。PI3K/mTOR Inhibitor-6 在人工胃液中的稳定性优于 gedatolisib。PI3K/mTOR Inhibitor-6 在 10 μM 时显着抑制 PI3K/Akt/mTOR 信号通路。PI3K/mTOR Inhibitor-6具有研究癌症疾病的潜力。

PI3K/mTOR Inhibitor-6

PI3K/mTOR Inhibitor-6 Chemical Structure

CAS No. : 2456295-59-1

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

* Please select Quantity before adding items.

生物活性

PI3K/mTOR Inhibitor-6 (Compound 19c) is a potent and dual inhibitor of PI3K/mTOR. PI3K/mTOR Inhibitor-6 displays better stability in artificial gastric fluids than gedatolisib. PI3K/mTOR Inhibitor-6 significantly suppresses the PI3K/Akt/mTOR signaling pathway at 10 μM. PI3K/mTOR Inhibitor-6 has the potential for the research of cancer diseases[1].

分子量

598.66

Formula

C30H34N10O4

CAS 号

2456295-59-1

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]. Wang L, et al. Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors. Eur J Med Chem. 2020 Oct 15;204:112637

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

eIF4E-IN-3

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。

eIF4E-IN-3 

eIF4E-IN-3 是一种有效的真核起始因子 4e (eIF4e) 抑制剂。eIF4E-IN-3 具有研究 eIF4e 依赖性疾病的潜力,包括癌症研究 (信息摘自专利 WO2021003157A1,化合物 485)。

eIF4E-IN-3

eIF4E-IN-3 Chemical Structure

CAS No. : 2573979-29-8

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

* Please select Quantity before adding items.

生物活性

eIF4E-IN-3 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e). eIF4E-IN-3 has the potential for researching eIF4e dependent diseases, including the research of cancer (extracted from patent WO2021003157A1, compound 485)[1].

IC50 & Target

eIF4e[1]

分子量

711.15

Formula

C34H30ClF3N6O4S

CAS 号

2573979-29-8

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]. Samuel Sperry, et al. Eif4e-inhibiting 4-oxo-3,4-dihydropyrido[3,4-d]pyrimidine compounds. Patent WO2021003157A1.

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

IMPDH2-IN-2

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。

IMPDH2-IN-2 

IMPDH2-IN-2 是一种有效的肌苷 5′-单磷酸脱氢酶 (IMPDH) 抑制剂,Ki,app 值分别为 14 μM。IMPDH2-IN-2 显示出中等的抗菌活性 (MIC = 6.3 和 11 μM,分别在最小 GAST/Fe 和丰富的 7H9/ADC/Tween 培养基中)。IMPDH2-IN-2 是一种潜在的抗结核药物。

IMPDH2-IN-2

IMPDH2-IN-2 Chemical Structure

CAS No. : 1434517-02-8

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

* Please select Quantity before adding items.

生物活性

IMPDH2-IN-2 is a potent inhibitor of inosine 5’-monophosphate dehydrogenase (IMPDH) with a Ki,app value of 14 μM, respectively. IMPDH2-IN-2 displays moderate antibacterial activity (MIC = 6.3 and 11 μM in minimal GAST/Fe and rich 7H9/ADC/Tween media, respectively). IMPDH2-IN-2 is a potential anti-tuberculosis agent[1].

IC50 & Target

IMPDH[1]

分子量

428.27

Formula

C21H15Cl2N3O3

CAS 号

1434517-02-8

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]. Chacko S, et al. Expanding Benzoxazole-Based Inosine 5′-Monophosphate Dehydrogenase (IMPDH) Inhibitor Structure-Activity As Potential Antituberculosis Agents [published correction appears in J Med Chem. 2021 Dec 23;64(24):18233-18234]. J Med Chem. 2018;61(11):4739-4756.

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

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt

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。

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt 

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt 对pre-miR-21 RNA 具有抑制活性。HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt 具有研究肿瘤疾病的潜力,例如癌症,尤其是表达 miR-21 的癌症 (信息提取自专利 2021087084A1,compound 25)。

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt Chemical Structure

CAS No. : 2641500-83-4

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

* Please select Quantity before adding items.

生物活性

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has inhibitory activity against pre-miR-21 RNA. HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has the potential for the research of neoplastic disease such as cancer and especially cancers expressing miR-21 (extracted from patent WO2021087084A1, compound 25)[1].

IC50 & Target

pre-miR-21 RNA[1]

分子量

1051.21

Formula

C57H62N8O10S

CAS 号

2641500-83-4

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]. Matthew D. Disney, et al. COMPOUNDS AND MODULES FOR INHIBITION OF PRE-miR-21 AND THEIR USE IN TREATMENT OF CERTAIN CANCERS. Patent WO2021087084A1.

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

KRAS inhibitor-14

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。

KRAS inhibitor-14 

KRAS inhibitor-14 (compound 3-22) 是一种有效的 KRAS G12C 抑制剂,IC50 为 0.249 µM。KRAS inhibitor-14 在 MIA PaCA-2,A549 细胞中显示出 p-ERK 抑制活性,IC50s 分别为 1.12,>33.3 µM。KRAS inhibitor-14 具有研究胰腺癌,结直肠癌和肺癌的潜力。

KRAS inhibitor-14

KRAS inhibitor-14 Chemical Structure

CAS No. : 2230873-78-4

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

* Please select Quantity before adding items.

生物活性

KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC50 of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC50s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers[1].

IC50 & Target[1]

KRas G12C

0.249 μM (IC50)

分子量

486.77

Formula

C20H15Cl3FN3O2S

CAS 号

2230873-78-4

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]. Brian alan, et al. KRAS g12c inhibitors and methods of using the same. WO2018119183 A2

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

ART615

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。

ART615 

ART615 是 ART558 的相关异构体。ART615 是 ART558 的不活跃形式,在 12 μM 时引起 <10% 的 Polθ 抑制,因此可作为 ART558 (IC50=7.9 nM) 的对照。

ART615

ART615 Chemical Structure

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

* Please select Quantity before adding items.

生物活性

ART615 is the related isomer of ART558. ART615, the inactive of ART558, elicits <10% Polθ inhibition at 12 µM, thus serving as a control for ART558 (IC50=7.9 nM)[1].

分子量

418.41

Formula

C21H21F3N4O2

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]. Zatreanu D, et al. Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance. Nat Commun. 2021 Jun 17;12(1):3636.

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

3,4-Dibromo-Mal-PEG2-amine TFA

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。

3,4-Dibromo-Mal-PEG2-amine TFA  纯度: ≥98.0%

3,4-Dibromo-Mal-PEG2-amine TFA 是一种 PROTAC linker,属于 PEG 类,可用于合成 PROTAC 分子。

3,4-Dibromo-Mal-PEG2-amine TFA

3,4-Dibromo-Mal-PEG2-amine TFA Chemical Structure

CAS No. : 2296708-07-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ¥2500 In-stock
10 mg ¥4000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

生物活性

3,4-Dibromo-Mal-PEG2-amine TFA is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target[1]

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

分子量

500.06

Formula

C12H15Br2F3N2O6

CAS 号

2296708-07-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°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 : 100 mg/mL (199.98 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9998 mL 9.9988 mL 19.9976 mL
5 mM 0.4000 mL 1.9998 mL 3.9995 mL
10 mM 0.2000 mL 0.9999 mL 1.9998 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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.00 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 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: ≥ 2.5 mg/mL (5.00 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.00 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.

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

Iruplinalkib(Synonyms: WX-0593)

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。

Iruplinalkib (Synonyms: WX-0593)

Iruplinalkib (WX-0593) 是一种有效的、选择性的、具有口服活性的 ALKROS1 酪氨酸激酶抑制剂。Iruplinalkib (WX-0593) 在伴有 ALK 或 ROS1 重排的晚期 NSCLC 中显示出良好的安全性和有希望的抗肿瘤活性。

Iruplinalkib(Synonyms: WX-0593)

Iruplinalkib Chemical Structure

CAS No. : 1854943-32-0

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

* Please select Quantity before adding items.

生物活性

Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and ROS1 tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement[1].

IC50 & Target

ALK and ROS1[1]

分子量

569.08

Formula

C29H38ClN6O2P

CAS 号

1854943-32-0

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]. Shi Y, et al. Safety and activity of WX-0593 (Iruplinalkib) in patients with ALK- or ROS1-rearranged advanced non-small cell lung cancer: a phase 1 dose-escalation and dose-expansion trial. Signal Transduct Target Ther. 2022;7(1):25.

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

Recoflavone(Synonyms: DA-6034 free acid)

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。

Recoflavone (Synonyms: DA-6034 free acid)

Recoflavone是一种合成的eupatilin衍生物,对胃粘膜有保护作用。Recoflavone具有治疗消化性溃疡的潜力。

Recoflavone(Synonyms: DA-6034 free acid)

Recoflavone Chemical Structure

CAS No. : 203191-10-0

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

* Please select Quantity before adding items.

生物活性

Recoflavone is a synthetic derivative of eupatilin that has a protective effect on gastric mucosa. Recoflavone has the potential to be used to treat peptic ulcer disease.

分子量

386.35

Formula

C20H18O8

CAS 号

203191-10-0

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]. Choi SM, Seo MJ, Lee YG, et al. Effects of DA-6034, a flavonoid derivative, on mucin-like glycoprotein and ocular surface integrity in a rabbit model. Arzneimittelforschung. 2009;59(10):498-503.

    [2]. Kwak DS, Lee OY, Lee KN, et al. The Effect of DA-6034 on Intestinal Permeability in an Indomethacin-Induced Small Intestinal Injury Model. Gut Liver. 2016;10(3):406-411.

    [3]. Kim YW, Lee WH, Choi SM, et al. DA6034 promotes gastric epithelial cell migration and wound-healing through the mTOR pathway. J Gastroenterol Hepatol. 2012;27(2):397-405.

    [4]. Nam SY, Kim JS, Kim JM, et al. DA-6034, a derivative of flavonoid, prevents and ameliorates dextran sulfate sodium-induced colitis and inhibits colon carcinogenesis. Exp Biol Med (Maywood). 2008;233(2):180-191.

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

PI3K/mTOR Inhibitor-7

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。

PI3K/mTOR Inhibitor-7 

PI3K/mTOR Inhibitor-7 (Compound 19i) 是一种有效的 PI3K/mTOR 双重抑制剂。PI3K/mTOR Inhibitor-7 的效力比阳性对照 gedatolisib 高 4.7 倍(0.3 对 1.4 μM,IC50 值)。PI3K/mTOR Inhibitor-7 在 10 μM 时显着抑制 PI3K/Akt/mTOR 信号通路。PI3K/mTOR Inhibitor-7 具有研究癌症疾病的潜力。

PI3K/mTOR Inhibitor-7

PI3K/mTOR Inhibitor-7 Chemical Structure

CAS No. : 2456295-65-9

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

* Please select Quantity before adding items.

生物活性

PI3K/mTOR Inhibitor-7 (Compound 19i) is a potent and dual inhibitor of PI3K/mTOR. PI3K/mTOR Inhibitor-7 shows 4.7-fold higher potency than the positive control gedatolisib (0.3 vs. 1.4 μM, IC50 values). PI3K/mTOR Inhibitor-7 significantly suppresses the PI3K/Akt/mTOR signaling pathway at 10 μM. PI3K/mTOR Inhibitor-7 has the potential for the research of cancer diseases[1].

分子量

571.63

Formula

C29H33N9O4

CAS 号

2456295-65-9

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]. Wang L, et al. Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors. Eur J Med Chem. 2020 Oct 15;204:112637

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

Amsilarotene(Synonyms: TAC-101; Am 555S)

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。

Amsilarotene (Synonyms: TAC-101; Am 555S) 纯度: 99.70%

Amsilarotene (TAC-101; Am 555S) 是一种具有口服活性的合成类视黄醇,对视黄酸受体 α (RAR-α) 具有选择性亲和力,对 RAR-α 和 RAR-β 的 Ki 值为 2.4 nM 和 400 nM。Amsilarotene 诱导人胃癌、肝细胞癌和卵巢癌细胞的凋亡 (apoptotic)。Amsilarotene 可用于癌症研究。

Amsilarotene(Synonyms: TAC-101;  Am 555S)

Amsilarotene Chemical Structure

CAS No. : 125973-56-0

规格 价格 是否有货 数量
5 mg ¥1800 In-stock
10 mg ¥2900 In-stock
25 mg ¥5800 In-stock
50 mg ¥9300 In-stock
100 mg ¥14500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Amsilarotene 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Transcription Factor Targeted Library
  • Anti-Liver Cancer Compound Library

生物活性

Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer[1][2][3].

IC50 & Target[1]

RARα

2.4 nM (Ki)

RARβ

400 nM (Ki)

体外研究
(In Vitro)

Amsilarotene (0, 10, 25 μM; 24 hours) induces apoptosis of human epithelial ovarian carcinoma-derived cell lines in a concentration-dependent manner[2].
Amsilarotene (10, 20 μM; 0, 3, 6, and 9 days) inhibits the proliferation of BxPC-3 and MIAPaCa-2 cells[3].
Amsilarotene (10 μM; 48 hours) increases the proportion of sensitive BxPC-3 cells in the G1 phase[3].
Amsilarotene (10 μM; 0, 3, 6, 24, 48, 72 hours) inhibits the retinoblastoma-gene product (RB) phosphorylation in BxPC-3 cells between 24 and 72 hours[3].

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

Apoptosis Analysis[2]

Cell Line: RMG-I, RMG-II, RTSG, RMUG-S, RMUG-L, and KF cells
Concentration: 0, 10, 25 μM
Incubation Time: 24 hours
Result: Induced apoptosis in a concentration-dependent manner in all of the cell lines, except KF cells.

Cell Proliferation Assay[3]

Cell Line: BxPC-3, MIAPaCa-2, AsPC-1 cells
Concentration: 10 and 20 μM
Incubation Time: 0, 3, 6, and 9 days.
Result: Inhibited the proliferation of BxPC-3 and MIAPaCa-2 cells, but not the proliferation of AsPC-1 cells.

Cell Cycle Analysis[3]

Cell Line: Sensitive BxPC-3 cells
Concentration: 10 μM
Incubation Time: 48 hours
Result: The proportion of cells in the G1 phase increased from 43% of untreated control cells to 86%

体内研究
(In Vivo)

Amsilarotene (8 mg/kg/day orally for 30 days) inhibits the RMG-II tumor growth in nude mice[2].

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

Animal Model: 6-week-old female BALB/c nu/nu mice with subcutaneous RMG-II tumors[2]
Dosage: 8 mg/kg/day
Administration: Orally for 30 days
Result: The maximal tumor growth-inhibiting effect was seen on day 31 of administration, when there was a 45% reduction of relative tumor volume (RTV).

分子量

385.60

Formula

C20H27NO3Si2

CAS 号

125973-56-0

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 : 100 mg/mL (259.34 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5934 mL 12.9668 mL 25.9336 mL
5 mM 0.5187 mL 2.5934 mL 5.1867 mL
10 mM 0.2593 mL 1.2967 mL 2.5934 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: ≥ 2.5 mg/mL (6.48 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.48 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 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: 2.5 mg/mL (6.48 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.48 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 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: ≥ 2.5 mg/mL (6.48 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.48 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]. Sun SY, et al. Differential effects of synthetic nuclear retinoid receptor-selective retinoids on the growth of human non-small cell lung carcinoma cells. Cancer Res. 1997 Nov 1;57(21):4931-9.

    [2]. Suzuki N, et al. A novel retinoid, 4-[3,5-bis (trimethylsilyl) benzamido] benzoic acid (TAC-101), induces apoptosis of human ovarian carcinoma cells and shows potential as a new antitumor agent for clear cell adenocarcinoma. Gynecol Oncol. 2004 Sep;94(3):643-9.

    [3]. Fujimoto K, et al. Induction of cell-cycle arrest and apoptosis by a novel retinobenzoic-acid derivative, TAC-101, in human pancreatic-cancer cells. Int J Cancer. 1999 May 17;81(4):637-44.

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

Sudocetaxel

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。

Sudocetaxel 

Sudocetaxel 是一种可以用于pH敏感的多西紫杉醇释放的微管解聚抑制剂。

Sudocetaxel

Sudocetaxel Chemical Structure

CAS No. : 1234218-62-2

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

* Please select Quantity before adding items.

生物活性

Sudocetaxel is a microtubule depolymerization inhibitor for pH-sensitive docetaxel delivery.

分子量

905.98

Formula

C48H59NO16

CAS 号

1234218-62-2

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]. Su Z, et al. Polymeric complex micelles based on the double-hydrazone linkage and dual drug-loading strategy for pH-sensitive docetaxel delivery. J Mater Chem B. 2016 Feb 14;4(6):1122-1133.

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

Palifosfamide tromethamine(Synonyms: Isophosphoramide mustard tromethamine; IPM tromethamine; ZIO-201 tromethamine)

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。

Palifosfamide tromethamine (Synonyms: Isophosphoramide mustard tromethamine; IPM tromethamine; ZIO-201 tromethamine)

Palifosfamide (tromethamine) 是一种具有潜在抗肿瘤活性的合成烷基化剂。作为异环磷酰胺 (ifosfamide) 稳定的活性代谢物,Palifosfamide (tromethamine) 通过GC碱基对不可逆地烷基化和交联DNA,导致了DNA复制的抑制,并最终导致细胞死亡。与异环磷酰胺相比,Palifosfamide (tromethamine)的毒性较小。

Palifosfamide tromethamine(Synonyms: Isophosphoramide mustard tromethamine; IPM tromethamine; ZIO-201 tromethamine)

Palifosfamide tromethamine Chemical Structure

CAS No. : 1070409-31-2

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

* Please select Quantity before adding items.

生物活性

Palifosfamide (tromethamine) is a synthetic alkylating agent with potential antineoplastic activity. As the stabilized active metabolite of ifosfamide, palifosfamide (tromethamine) irreversibly alkylates and crosslinks DNA through GC base pairs. This leads to an inhibition of DNA replication and ultimately cell death. Compared to ifosfamide, palifosfamide (tromethamine) is less toxic.

分子量

342.16

Formula

C8H22Cl2N3O5P

CAS 号

1070409-31-2

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]. Jones B, Komarnitsky P, Miller GT, Amedio J, Wallner BP. Anticancer activity of stabilized palifosfamide in vivo: schedule effects, oral bioavailability, and enhanced activity with docetaxel and doxorubicin. Anticancer Drugs. 2012;23(2):173-184.

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

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt

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。

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt 

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt 对pre-miR-21 RNA 具有抑制活性。HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt 具有研究肿瘤疾病的潜力,例如癌症,尤其是表达 miR-21 的癌症 (信息提取自专利 2021087084A1,compound 25)。

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt Chemical Structure

CAS No. : 2641500-83-4

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

* Please select Quantity before adding items.

生物活性

HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has inhibitory activity against pre-miR-21 RNA. HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has the potential for the research of neoplastic disease such as cancer and especially cancers expressing miR-21 (extracted from patent WO2021087084A1, compound 25)[1].

IC50 & Target

pre-miR-21 RNA[1]

分子量

1051.21

Formula

C57H62N8O10S

CAS 号

2641500-83-4

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]. Matthew D. Disney, et al. COMPOUNDS AND MODULES FOR INHIBITION OF PRE-miR-21 AND THEIR USE IN TREATMENT OF CERTAIN CANCERS. Patent WO2021087084A1.

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

Sudocetaxel zendusortide

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。

Sudocetaxel zendusortide 

Sudocetaxel zendusortide 是一种抗肿瘤药。

Sudocetaxel zendusortide

Sudocetaxel zendusortide Chemical Structure

CAS No. : 2473125-34-5

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

* Please select Quantity before adding items.

生物活性

Sudocetaxel zendusortide is an antineoplastic[1].

分子量

3704.03

Formula

C₁₇₉H₂₄₈N₂₈O₅₇

CAS 号

2473125-34-5

Sequence Shortening

Ac-GVRAKAGVRN-{Nle}-FKSESY

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]. WHO Drug Information, Vol. 35, No. 4, 2021. International Nonproprietary Names for Pharmaceutical Substances (INN).

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

KRAS inhibitor-16

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。

KRAS inhibitor-16 

KRAS inhibitor-16 (compound 3-11) 是一种有效的 KRAS G12C 抑制剂,IC50 为 0.457 µM。KRAS inhibitor-16 在 MIA PaCA-2,A549 细胞中显示出 p-ERK 抑制活性,IC50s 分别为 3.06,11.1 µM。 KRAS inhibitor-16 具有研究胰腺癌,结直肠癌和肺癌的潜力。

KRAS inhibitor-16

KRAS inhibitor-16 Chemical Structure

CAS No. : 2230873-67-1

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

* Please select Quantity before adding items.

生物活性

KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC50 of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC50s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers[1].

IC50 & Target

KRas G12C

0.457 μM (IC50)

分子量

452.33

Formula

C20H16Cl2FN3O2S

CAS 号

2230873-67-1

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]. Brian Alan LANMAN, et al. Kras g12c inhibitors and methods of using the same. US20180334454A1.

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

C2 Ceramide (d14:1/2:0)

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。

C2 Ceramide (d14:1/2:0) 

C2 Ceramide (d14:1/2:0) 是一种用于诊断与环氧合酶 2 (COX2) 过度表达相关的疾病的组合物。C2 Ceramide (d14:1/2:0) 对 COX2 蛋白具有很强的结合活性 (信息提取自专利 WO2019235824A1)。

C2 Ceramide (d14:1/2:0)

C2 Ceramide (d14:1/2:0) Chemical Structure

CAS No. : 2097561-20-9

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

* Please select Quantity before adding items.

生物活性

C2 Ceramide (d14:1/2:0) is a composition for diagnosing diseases associated with cyclooxygenase 2 (COX2) overexpression. C2 Ceramide (d14:1/2:0) exhibits a strong binding activity to COX2 protein (extracted from patent WO2019235824A1).

分子量

285.42

Formula

C16H31NO3

CAS 号

2097561-20-9

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]. Composition for diagnosing diseases associated with cox2 overexpression and screening method therefor. Patent WO2019235824A1.

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

Iruplinalkib(Synonyms: WX-0593)

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。

Iruplinalkib (Synonyms: WX-0593)

Iruplinalkib (WX-0593) 是一种有效的、选择性的、具有口服活性的 ALKROS1 酪氨酸激酶抑制剂。Iruplinalkib (WX-0593) 在伴有 ALK 或 ROS1 重排的晚期 NSCLC 中显示出良好的安全性和有希望的抗肿瘤活性。

Iruplinalkib(Synonyms: WX-0593)

Iruplinalkib Chemical Structure

CAS No. : 1854943-32-0

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

* Please select Quantity before adding items.

生物活性

Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and ROS1 tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement[1].

IC50 & Target

ALK and ROS1[1]

分子量

569.08

Formula

C29H38ClN6O2P

CAS 号

1854943-32-0

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]. Shi Y, et al. Safety and activity of WX-0593 (Iruplinalkib) in patients with ALK- or ROS1-rearranged advanced non-small cell lung cancer: a phase 1 dose-escalation and dose-expansion trial. Signal Transduct Target Ther. 2022;7(1):25.

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

DHA-paclitaxel(Synonyms: Taxoprexin; Docosahexaenoic acid-paclitaxel)

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。

DHA-paclitaxel (Synonyms: Taxoprexin; Docosahexaenoic acid-paclitaxel)

DHA-paclitaxel是一种由天然脂肪酸DHA共价连接到紫杉醇的C2′-位置组成的惰性前药。紫杉醇部分与微管蛋白结合,抑制微管的分解,从而抑制细胞分裂。与紫杉醇相比,DHA-paclitaxel更特异性地靶向肿瘤细胞,因为肿瘤细胞吸收大量天然脂肪酸作为生化前体和能量来源。

DHA-paclitaxel(Synonyms: Taxoprexin;  Docosahexaenoic acid-paclitaxel)

DHA-paclitaxel Chemical Structure

CAS No. : 199796-52-6

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

* Please select Quantity before adding items.

生物活性

DHA-paclitaxel is an inert prodrug composed of the natural fatty acid DHA covalently linked to the C2′-position of paclitaxel. The paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Compared to Paclitaxel, DHA-Paclitaxel targets tumor cells more specifically because tumor cells absorb large amounts of natural fatty acids for use as biochemical precursors and energy sources.

分子量

1164.38

Formula

C69H81NO15

CAS 号

199796-52-6

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]. Sparreboom A, Wolff AC, Verweij J, et al. Disposition of docosahexaenoic acid-paclitaxel, a novel taxane, in blood: in vitro and clinical pharmacokinetic studies. Clin Cancer Res. 2003;9(1):151-159.

    [2]. Bradley MO, Webb NL, Anthony FH, et al. Tumor targeting by covalent conjugation of a natural fatty acid to paclitaxel. Clin Cancer Res.

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

Sudocetaxel

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。

Sudocetaxel 

Sudocetaxel 是一种可以用于pH敏感的多西紫杉醇释放的微管解聚抑制剂。

Sudocetaxel

Sudocetaxel Chemical Structure

CAS No. : 1234218-62-2

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

* Please select Quantity before adding items.

生物活性

Sudocetaxel is a microtubule depolymerization inhibitor for pH-sensitive docetaxel delivery.

分子量

905.98

Formula

C48H59NO16

CAS 号

1234218-62-2

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]. Su Z, et al. Polymeric complex micelles based on the double-hydrazone linkage and dual drug-loading strategy for pH-sensitive docetaxel delivery. J Mater Chem B. 2016 Feb 14;4(6):1122-1133.

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