DM4-d6

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。

DM4-d6 

DM4-d6 是 DM4 氘代物。DM4 是抑制细胞分裂的抗微管蛋白剂。DM4 可用于制备抗体药物偶联物。

DM4-d6

DM4-d6 Chemical Structure

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生物活性

DM4-d6 is deuterium labeled DM4. DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

分子量

786.40

Formula

C38H48D6ClN3O10S

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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Tang R, et al. P-gp activity is a critical resistance factor against AVE9633 and DM4 cytotoxicity in leukaemia cell lines, but not a major mechanism of chemoresistance in cells from acute myeloid leukaemia patients. BMC Cancer. 2009 Jun 23;9:199.

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Duocarmycin DM free base

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。

Duocarmycin DM free base  纯度: 98.11%

Duocarmycin DM free base 是一种 DNA 小沟烷基化剂 (DNA minor-groove alkylator),是一种抗体药物结合物 (ADCs) 毒素。Duocarmycin DM free base 因特有的结构而具有抗癌活性。

Duocarmycin DM free base

Duocarmycin DM free base Chemical Structure

CAS No. : 1116745-06-2

规格 价格 是否有货 数量
5 mg ¥8800 In-stock
10 mg ¥14000 In-stock
25 mg ¥28000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Duocarmycin DM free base 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Toxins for Antibody-Drug Conjugate Research Library

生物活性

Duocarmycin DM free base, a DNA minor-groove alkylator, is an antibody drug conjugates (ADCs) toxin. Duocarmycin DM free base is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity[1][2].

IC50 & Target[1]

Daunorubicins/Doxorubicins

 

体外研究
(In Vitro)

The Duocarmycins and CC-1065 are members of a class of DNA minor groove, AT-sequence selective, and adenine-N3 alkylating agents, isolated from Streptomyces sp. that exhibit extremely potent cytotoxicity against the growth of cancer cells grown in culture[2].
Duocarmycin shows cytotoxicity to several human cancer cells, with IC50 of 22, 13.8, 3.87, 15.4, and 7.31 pM for HT-29, CL1-5, Caski, EJ, and LS174T, respectively[3].

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

463.96

Formula

C26H26ClN3O3

CAS 号

1116745-06-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (107.77 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1554 mL 10.7768 mL 21.5536 mL
5 mM 0.4311 mL 2.1554 mL 4.3107 mL
10 mM 0.2155 mL 1.0777 mL 2.1554 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 (protect from light, stored under nitrogen)。-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]. Patil PC, et al. A Short Review on the Synthetic Strategies of Duocarmycin Analogs that are Powerful DNA Alkylating Agents. Anticancer Agents Med Chem. 2015;15(5):616-630.

    [2]. Koch MF, et al. Structural, Biochemical, and Computational Studies Reveal the Mechanism of Selective Aldehyde Dehydrogenase 1A1 Inhibition by Cytotoxic Duocarmycin Analogues. Angew Chem Int Ed Engl. 2015 Nov 9;54(46):13550-4.

    [3]. Chen KC, et al. Selective cancer therapy by extracellular activation of a highly potent glycosidic duocarmycin analogue. Mol Pharm. 2013;10(5):1773-1782.

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DBA-DM4

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。

DBA-DM4 

DBA-DM4 是 drug-linker conjugate,由 linker DBA 和 毒性分子 DM4 连接而成的,可用来制备抗体偶联药物。DM4 是抑制细胞分裂的抗微管蛋剂。

DBA-DM4

DBA-DM4 Chemical Structure

CAS No. : 905449-84-5

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生物活性

DBA-DM4 is a drug-linker conjugate composed of a potent a tubulin inhibitor DM1 and a linker SPDP to make antibody drug conjugate (ADC)[1].

IC50 & Target

Maytansinoids

 

分子量

898.52

Formula

C42H60ClN3O12S2

CAS 号

905449-84-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [1]. Samantha Congreve, et al. Antibody drug conjugates (ADC) Current status and mapping of ADC:s in clinical programs

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LDN193189(Synonyms: DM-3189)

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。

LDN193189 (Synonyms: DM-3189) 纯度: 99.42%

LDN193189 (DM-3189) 是一种选择性的 BMP I 型受体抑制剂,抑制 ALK2ALK3IC50 分别为 5 nM 和 30 nM。对 ALK4,ALK5 和 ALK7 的作用效果弱 (IC50≥500 nM)。

LDN193189(Synonyms: DM-3189)

LDN193189 Chemical Structure

CAS No. : 1062368-24-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
2 mg ¥700 In-stock
5 mg ¥950 In-stock
10 mg ¥1600 In-stock
50 mg ¥6000 In-stock
100 mg   询价  
200 mg   询价  

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LDN193189 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

LDN193189 (DM-3189) is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM)[1].

IC50 & Target[1]

ALK2

5 nM (IC50)

ALK3

30 nM (IC50)

体外研究
(In Vitro)

LDN193189 inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with greater potency than did dorsomorphin (IC50=5 nM versus 470 nM) while retaining 200-fold selectivity for BMP signaling versus TGF-β signaling (IC50 for TGF-β ≥1,000 nM). LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), and the TGF-β type I receptors ALK4, ALK5 and ALK7 (IC50≥500 nM) and increases selectivity for BMP signaling versus AMP-activated protein kinase, PDGFR and MAPK signaling pathways as compared to the parent compound. LDN-193189 blocks the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins. These findings suggest that LDN193189 might affect BMP-induced osteoblast differentiation. In fact, LDN193189 inhibits the induction of alkaline phosphatase activity in C2C12 cells by BMP4 even when administered 12 h after BMP stimulation, indicating sustained BMP signaling activity is needed for osteogenic differentiation[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)

In the first experiment, LDN193189 (3 mg/kg) is injected intraperitoneally twice a day after tumors became palpable 7 days post-implantation. The growth rates between the control vehicle- and LDN193189-treated mice are not significantly different after the first 5 weeks, but differences in the growth rates are detected after 6 and 7 weeks post-treatment. In the second experiment, cells are isolated from PCa-118b tumors and injected subcutaneously into SCID mice (1×106 cells per mouse). LDN193189 or vehicle is applied to mice 5 days post-tumor cell injection before tumors are palpable. The differences in the average growth rates between these two groups, as measured by tumor size, are significant at 6 and 7 weeks post-treatment. The tumor weights also show significant differences at the termination of the study at week 7. The X-ray of the tumors shows that the ectopic bone volume and bone density are reduced in the tumors of LDN193189-treated group compared to that of controls[2]. Co-incubation of pulmonary arterial smooth muscle cells (PASMCs) from the pulmonary arterial hypertension (PAH) rats with UK-92480 and LDN193189 completely inhibited the anti-proliferation and up-regulation of the bone morphogenetic protein (BMPR2) and Cx40 expression by the UK-92480[3].

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

406.48

Formula

C25H22N6

CAS 号

1062368-24-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 12 mg/mL (29.52 mM; ultrasonic and adjust pH to 2 with HCl)

Ethanol : 1 mg/mL (2.46 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 2.4601 mL 12.3007 mL 24.6015 mL
5 mM 0.4920 mL 2.4601 mL 4.9203 mL
10 mM 0.2460 mL 1.2301 mL 2.4601 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: ≥ 1.2 mg/mL (2.95 mM); Clear solution

    此方案可获得 ≥ 1.2 mg/mL (2.95 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.0 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: ≥ 1.2 mg/mL (2.95 mM); Clear solution

    此方案可获得 ≥ 1.2 mg/mL (2.95 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.0 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]. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369.

    [2]. Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis. Cancer Res, 2011, 71(15), 5194-5203.

    [3]. Yang L, et al. UK-92480 increases connexin 40 in smooth muscle cells through activation of BMP pathways in pulmonary arterial hypertension. Int J Clin Exp Pathol. 2014 Jul 15;7(8):4674-84.

Cell Assay
[1]

Mouse PASMCs grown are transiently transfected to 50% confluence in six-well plates with 0.3 μg Id1promoter luciferase reporter construct (BRE-Luc) in combination with 0.6 μg of plasmid expressing constitutively active forms of BMP type I receptors (caALK2, caALK3 or caALK6). For both reporter plasmids, 0.2 μg of pRL-TKRenilla luciferase are used to control for transfection efficiency. PASMCs are incubated with LDN193189 (2 nM-32 μM) or vehicle starting 1 h after transfection. Cell extracts are harvested and quantified relative promoter activity by the ratio of firefly to Renilla luciferase activity with the dual luciferase assay kit.

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][3]

Mice[2]
In the first experiment, SCID mice are implanted with MDA-PCa-118b tumors. After 7 days when tumors reached measurable sizes, mice are injected with LDN193189 (3 mg/kg) or with vehicle intraperitoneally twice a day. Tumor sizes and body weights are measured weekly. Mice are injected with calcein at three days and one day prior to sacrifice. Blood is collected and tumors are weighed. A portion of the tumors are fixed in formaldehyde for micro-computed tomography (microCT), using EVS CT, or further decalcified for bone histomorphometric analysis, using OsteoMeasure Analysis System, or flash frozen for RNA preparation. Osteocalcin in the mouse serum is determined by ELISA. In the second experiment, PCa-118b tumors are first digested with Accumax, and the isolated cells are plated overnight, resuspended in Matrigel in 1:1 ratio, and injected into SCID mice (1×106 cells/mouse) subcutaneously. Mice are treated with LDN193189 five days post-injection.
Rats[3]
Male Sprague-Dawley (SD) rats, 8 weeks of age, weighing 200-220 g, are purchased from Nanjing Medical University animal center. Rats are randomly assigned to one of seven experiment groups (n=6 per group). Rats are housed with free access to food and water under a natural 12/12 h day/night cycle. The Monocrotaline is administered (60 mg/kg) to rats by subcutaneous injection into the back region. The animal’s lungs are harvested at 28th day of the study after hemodynamic assessment. The UK-92480 group received daily intragastric administration of UK-92480 after the administration of MCT (60 mg/kg). The LDN193189 group received daily intragastric administration of UK-92480 (50 mg/kg) and intraperitoneal injection of LDN193189 (10 mg/kg). In other groups, the same volume saline is given.

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]. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369.

    [2]. Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis. Cancer Res, 2011, 71(15), 5194-5203.

    [3]. Yang L, et al. UK-92480 increases connexin 40 in smooth muscle cells through activation of BMP pathways in pulmonary arterial hypertension. Int J Clin Exp Pathol. 2014 Jul 15;7(8):4674-84.

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大龙(医疗) 低速离心机DM0412

大龙(医疗) 低速离心机DM0412

  • 品牌 大龙|DLAB
  • 型号 DM0412(医疗)
  • 货号 9025101121
  • 商品详情

    产品介绍:

    国际安全认证:通过及其严格的欧盟EN61010-2-20离心机特殊安全标准——爆炸测试,获得极具公信力的TUV德国莱茵公司颁发的CE, cTUVus和FCC国际安全产品认证。

    通过欧盟EN61010-2-101:2002 医疗产品体外诊断用医疗器械指令(IVD);

    安全裕度大,噪音低:高强度塑料合金转子以及优良的动平衡技术,保证机器超低音稳定运行;

    30秒-99分钟定时和连续运行两种操作模式;

    合理的刹车曲线,保证样品没有混淆,分离效果更好;

    用户友好型LCD大显示屏;

    达到设定转速后,可修改运行参数;

    离心完毕后,声音提示并自动开盖,便于样品降温;

    运行进程显示和错误代码提示。

    技术参数:

    技术参数 DM0412
    最高转速(rpm) 300-4500,步进:100
    最大相对离心力(×g ) 2490×g, 步进:100×g
    转速精度(rpm) ±20
    定时 30秒-99分-HOLD (连续运行)
    驱动电机 直流无刷电机
    显示屏 LCD
    安全性能 门锁,过温保护,过速保护,状态诊断系统
    电源 单相, 110V-240V, 50Hz/60Hz, 3A
    噪音(dB) ≤56
    加减速度 A12-10P: 20s↑13s↓
    A6-50P: 20s↑20 s /90s↓
    尺寸(长x宽x高) 354×301×217mm
    重量 6 kg
    认证 CE, UL, IVD
    强化功能 转速/相对离心力转换功能、瞬时离心功能、
    声音提示功能、运行进程显示
    产品编号 型号 描述
    9034002122 DM0412 低速离心机(含A12-10P塑料转子),国标插头,110V-240V/50Hz/60Hz
    转子
    19200316 A12-10P 塑料转子,最高转速 4500rpm,最大容量10ml x 12,适用于DM0412
    转子适配器
    19200348 A12-10P 塑料转子,最高转速 4500rpm,最大容量15ml x 8,适用于DM0412
    19400027 A10P15 转子适配器, 适用于A12-10P转子, 12pcs/pk
    19400028 转子适配器垫块,可与A10P15配套使用,12pcs/pk

  • 大龙毛细管离心机DM1424

    大龙毛细管离心机DM1424

  • 品牌 大龙|DLAB
  • 型号 DM1424
  • 货号 9033001124
  • 商品详情

    产品介绍:

    转速200-14000rpm,相对离心力18620×g,转速和离心力可切换显示;

    转速和时间高精度控制,分离效果更好;

    LCD显示屏,可实时显示运行参数;

    直流无刷电机,免维护,安全,转速控制精准;

    瞬时离心功能,扩展了产品的应用;

    电子锁设计,离心结束后自动开盖,节省时间同时防止样品过热;

    开机自检,显示累计运行时间和上次运行参数;

    最大转子能力:角转子2mL×24 最大转速:14000rpm;毛细管转子:24根毛细管 最大转速12000rpm;

    可选配角转子,实现一机两用。

    技术参数:

    技术参数 DM1424  
    最高转速[rpm] 200-14000,步进:10
    最大相对离心力[xg] 18620×g,步进:10×g
    转速精度 ±30
    最大容量 1.5/2ml×24 (14000rpm);
    毛细管转子-24根毛细管(12000rpm)
    定时 30秒-99分-HOLD (连续运行)
    驱动电机 直流无刷电机
    显示屏 LCD
    安全性能 双门锁,过温保护,过速保护,状态诊断系统,转子识别
    电源 单相, 200V-240V, 50Hz/60Hz, 5A;100V-120V, 50Hz/60Hz, 5A
    噪音(dB) ≤60
    加减速度 20s↑20s↓
    尺寸(毫米) (L)280×(W)364×(H)266
    重量 10kg
    其它功能 转速/离心力转换功能,瞬时离心功能,运行进程显示,声音提示功能

    货号 型号 描述
     
    9033001124  DM1424 毛细管离心机(含AC24P毛细管转子套装),国标插头,220V-240V/50Hz/
    60Hz
    转子
    19400014 AC24P 毛细管转子套装,含转子、转子盖和读数盘 (DragonLabLOGO),最高转速12000rpm,最大容量24根毛细管,适用于DM1424
    19400019 A24-2P 塑料转子套(DragonLab
     LOGO),最高转速14000
    rpm,最大容量2ml x 24,适用于DM1424
    转子适配器
    19500001 A02P2 2ml转0.2ml转子适配器,用A12-2,A12-2P,AS24-2和A24-2P 转子24pcs/pk
    19500002 A05P2 2ml转0.5ml转子适配器,适用于A12-2,A12-2P,
    AS24-2和A24-2P 转子,24pcs/pk

  • Mertansine(Synonyms: DM1; Maytansinoid DM1)

    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。

    Mertansine (Synonyms: DM1; Maytansinoid DM1) 纯度: 99.80%

    Mertansine (DM1) 是一种微管蛋白抑制剂,也是一种抗体可缀合的美登木素生物碱,用于克服与美登素相关的全身毒性并增强肿瘤特异性递送。Mertansine 可以通过连接体连接到单克隆抗体上,形成抗体偶联药物(ADC)。

    Mertansine(Synonyms: DM1;  Maytansinoid DM1)

    Mertansine Chemical Structure

    CAS No. : 139504-50-0

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    Free Sample (0.1-0.5 mg)   Apply now  
    2 mg ¥550 In-stock
    5 mg ¥880 In-stock
    10 mg ¥1500 In-stock
    25 mg ¥3000 In-stock
    50 mg ¥5200 In-stock
    100 mg ¥9400 In-stock
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    Mertansine 相关产品

    相关化合物库:

    • Drug Repurposing Compound Library Plus
    • Clinical Compound Library Plus
    • Bioactive Compound Library Plus
    • Toxins for Antibody-Drug Conjugate Research Library
    • Peptidomimetic Library

    生物活性

    Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC)[1][2].

    IC50 & Target

    Maytansinoids

     

    Clinical Trial

    分子量

    738.29

    Formula

    C35H48ClN3O10S

    CAS 号

    139504-50-0

    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

    *该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    溶解性数据
    In Vitro: 

    DMSO : 62.5 mg/mL (84.66 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.3545 mL 6.7724 mL 13.5448 mL
    5 mM 0.2709 mL 1.3545 mL 2.7090 mL
    10 mM 0.1354 mL 0.6772 mL 1.3545 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;该产品在溶液状态不稳定,建议您现用现配,即刻使用

    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: 2.17 mg/mL (2.94 mM); Suspended solution; Need ultrasonic

      此方案可获得 2.17 mg/mL (2.94 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 21.7 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    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (2.82 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (2.82 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

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (2.82 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (2.82 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]. Manu Lopus et al. Maytansine and Cellular Metabolites of Antibody-Maytansinoid Conjugates Strongly Suppress Microtubule Dynamics by Binding to Microtubules.

      [2]. Lopus M. Antibody-DM1 conjugates as cancer therapeutics. Cancer Lett. 2011 Aug 28;307(2):113-8.

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    Ganoderic acid DM(Synonyms: 灵芝酸 DM)

    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。

    Ganoderic acid DM (Synonyms: 灵芝酸 DM) 纯度: 99.65%

    Ganoderic acid DM 是可从 Ganoderma lucidum 分离得到的一个天然三萜,可诱导人乳腺癌细胞的 DNA 损伤、G1 细胞周期阻滞和凋亡。Ganoderic acid DM 还是破骨形成的特异性抑制剂。

    Ganoderic acid DM(Synonyms: 灵芝酸 DM)

    Ganoderic acid DM Chemical Structure

    CAS No. : 173075-45-1

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    5 mg ¥11600 In-stock
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    Ganoderic acid DM 相关产品

    相关化合物库:

    • Natural Product Library Plus
    • Bioactive Compound Library Plus

    生物活性

    Ganoderic acid DM, a natural triterpenoid isolated from Ganoderma lucidum, induces DNA damage, G1 cell cycle arrest and apoptosis in human breast cancer cells. Ganoderic acid DM as a specific inhibitor of osteoclastogenesis[1][2].

    体外研究
    (In Vitro)

    Ganoderic acid DM (GADM) effectively inhibits cell proliferation and colony formation in MCF-7 human breast cancer cells, which was much stronger than that of MDA-MB-231 breast cancer cells[1].
    Ganoderic acid DM especially suppresses the expression of c-Fos and nuclear factor of activated T cells c1 (NFATc1). Ganoderic acid DM markedly suppressed the expression of cathepsin K and TRAP mRNA[2].
    Ganoderic acid DM induces autophagic apoptosis in non-small cell lung cancer cells by inhibiting the PI3K/Akt/mTOR activity[3].

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

    Cell Viability Assay[1]

    Cell Line: MCF-7 and MDA-MB-231 cells.
    Concentration: 0-100 μM.
    Incubation Time: 48 h.
    Result: Decreased the cell viability in breast cancer cells.

    Cell Viability Assay[2]

    Cell Line: RAW-D cells.
    Concentration: 0-100 μg/mL.
    Incubation Time: 0-100 μg/mL.
    Result: Clearly suppressed osteoclastogenesis from the RAW 264 cell D-clone.

    分子量

    468.67

    Formula

    C30H44O4

    CAS 号

    173075-45-1

    中文名称

    灵芝酸 DM

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

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

    参考文献
    • [1]. Guo-Sheng Wu, et al. Ganoderic acid DM, a natural triterpenoid, induces DNA damage, G1 cell cycle arrest and apoptosis in human breast cancer cells. Fitoterapia. 2012 Mar;83(2):408-14.

      [2]. Ichiko Miyamoto, et al. Regulation of osteoclastogenesis by ganoderic acid DM isolated from Ganoderma lucidum. Eur J Pharmacol. 2009 Jan 5;602(1):1-7.

      [3]. Junbo Xia, et al. Ganoderic acid DM induces autophagic apoptosis in non-small cell lung cancer cells by inhibiting the PI3K/Akt/mTOR activity. Chem Biol Interact. 2020 Jan 25;316:108932.

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    SMCC-DM1(Synonyms: DM1-SMCC)

    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。

    SMCC-DM1 (Synonyms: DM1-SMCC) 纯度: 98.18%

    SMCC-DM1 (DM1-SMCC) 是由 linker SMCC 和 毒性分子 DM1 连接而成的,可用来制备抗体偶联药物。DM1 (Mertansine),是含硫醇的美登木素生物碱,是一种有效的微管破坏剂。

    SMCC-DM1(Synonyms: DM1-SMCC)

    SMCC-DM1 Chemical Structure

    CAS No. : 1228105-51-8

    规格 价格 是否有货 数量
    5 mg ¥3300 In-stock
    10 mg ¥5100 In-stock
    25 mg ¥9900 In-stock
    50 mg ¥15500 In-stock
    100 mg ¥22000 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    生物活性

    SMCC-DM1 (DM1-SMCC) is a drug-linker conjugate composed of a potent microtubule-disrupting agent DM1 and a linker SMCC to make antibody drug conjugate (ADC)[1].

    IC50 & Target

    Maytansinoids

     

    体外研究
    (In Vitro)

    SMCC-DM1 inhibits HCC1954 and MDA-MB-468 cells proliferation with IC50s of 17.2 and 49.9 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

    1072.61

    Formula

    C51H66ClN5O16S

    CAS 号

    1228105-51-8

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    溶解性数据
    In Vitro: 

    DMSO : ≥ 100 mg/mL (93.23 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 0.9323 mL 4.6615 mL 9.3231 mL
    5 mM 0.1865 mL 0.9323 mL 1.8646 mL
    10 mM 0.0932 mL 0.4662 mL 0.9323 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 (stored under nitrogen)。-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 mg/mL (1.86 mM); Clear solution; Need ultrasonic

      此方案可获得 2 mg/mL (1.86 mM) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.0 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 mg/mL (1.86 mM); Clear solution; Need ultrasonic

      此方案可获得 2 mg/mL (1.86 mM) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.0 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 mg/mL (1.86 mM); Clear solution

      此方案可获得 ≥ 2 mg/mL (1.86 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 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Shao S, et al. Site-specific and hydrophilic ADCs through disulfide-bridged linker and branched PEG. Bioorg Med Chem Lett. 2018 May 1;28(8):1363-1370.

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    Sulfo-PDBA-DM4

    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。

    Sulfo-PDBA-DM4 

    Sulfo-PDBA-DM4 是 drug-linker conjugate,由 linker Sulfo-PDBA 和 毒性分子 DM4 连接而成的,可用来制备抗体偶联药物。Sulfo-PDBA 是一种谷氨酸可降解 (cleavable) 的 linker。

    Sulfo-PDBA-DM4

    Sulfo-PDBA-DM4 Chemical Structure

    CAS No. : 1461704-01-7

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

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    生物活性

    Sulfo-PDBA-DM4 is a drug-linker conjugate composed of a potent a tubulin inhibitor DM4 and a linker Sulfo-PDBA to make antibody drug conjugate (ADC). Sulfo-PDBA is a gluthatione cleavable linker.

    IC50 & Target

    Maytansinoids

     

    分子量

    978.58

    Formula

    C42H60ClN3O15S3

    CAS 号

    1461704-01-7

    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]. Sun X, et al. Effects of Drug-Antibody Ratio on Pharmacokinetics, Biodistribution, Efficacy, and Tolerability of Antibody-Maytansinoid Conjugates. Bioconjug Chem. 2017 May 17;28(5):1371-1381.

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    DM4-SMCC

    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。

    DM4-SMCC 

    DM4-SMCC 是一种抗体偶联药物 (drug-linker conjugate for ADC),具有抗肿瘤活性,由抗微管抑制剂 DM4 和不可降解 (non-cleavable) 的 SMCC 连接而成。

    DM4-SMCC

    DM4-SMCC Chemical Structure

    CAS No. : 1228105-52-9

    规格 价格 是否有货
    10 mg ¥22990 询问价格 & 货期
    25 mg ¥45980 询问价格 & 货期
    50 mg ¥80460 询问价格 & 货期

    * Please select Quantity before adding items.

    生物活性

    DM4-SMCC is a drug-linker conjugate for ADC with antitumor activity by using DM4 (an antitubulin agent), linked via the non-cleavable SMCC linker[1].

    IC50 & Target

    Maytansinoids

     

    分子量

    1114.69

    Formula

    C54H72ClN5O16S

    CAS 号

    1228105-52-9

    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]. Singh R, et al. A New Triglycyl Peptide Linker for Antibody-Drug Conjugates (ADCs) with Improved TargetedKilling of Cancer Cells. Mol Cancer Ther. 2016 Jun;15(6):1311-20.

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    SPP-DM1

    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。

    SPP-DM1 

    SPP-DM1 是抗体偶联药物的一部分,由微管破坏剂 DM1 和 ADC linker SPP 连接而成。

    SPP-DM1

    SPP-DM1 Chemical Structure

    CAS No. : 452072-20-7

    规格 价格 是否有货
    10 mg ¥22990 询问价格 & 货期
    25 mg ¥45980 询问价格 & 货期
    50 mg ¥80460 询问价格 & 货期

    * Please select Quantity before adding items.

    生物活性

    SPP-DM1 is a drug-linker conjugate for ADC with potent antitumor activity by using DM1 (a potent microtubule-disrupting agent), linked via the ADC linker SPP[1].

    IC50 & Target

    Maytansinoids

     

    分子量

    967.54

    Formula

    C44H59ClN4O14S2

    CAS 号

    452072-20-7

    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]. Manu Lopus et al. Maytansine and Cellular Metabolites of Antibody-Maytansinoid Conjugates Strongly Suppress Microtubule Dynamics by Binding to Microtubules.

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    S-methyl DM1

    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。

    S-methyl DM1 

    S-methyl DM1 是一种美登素 (Maytansine) 的硫代甲基衍生物。S-methyl DM1 以 Kd 为 0.93 μM 结合微管蛋白并抑制微管聚合。S-methyl DM1 可以有效抑制微管动态不稳定性,并具有抗癌作用。

    S-methyl DM1

    S-methyl DM1 Chemical Structure

    CAS No. : 912569-84-7

    规格 是否有货
    500 μg 询价
    1 mg 询价

    * Please select Quantity before adding items.

    生物活性

    S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects[1][2].

    IC50 & Target

    Maytansinoids

     

    体外研究
    (In Vitro)

    S-methyl DM1 is the primary cellular or liver metabolite of antibody-maytansinoid conjugates prepared with thiol-containing maytansinoids DM1[1].
    The half-maximal concentration for inhibition of microtubule assembly for for S-methyl DM1 is 4 μM. At 100 nM S-methyl-DM1 (84%) suppresses dynamic instability more strongly than Maytansine (45%). Tritiated S-methyl-DM1 bound to 37 high-affinity sites per microtubule (Kd of 0.1 μM)[1].
    The concentration dependence curves for the inhibition of cell proliferation by S-methyl DM1 is sigmoidal in shape in MCF7 cells. Minimal inhibition occurred at 200 pM S-methyl DM1, and inhibition is maximal at 3 nM. S-methyl DM1 (IC50 of 330 pM) is slightly more potent than Maytansine (IC50 of 710 pM)[2].
    S-methyl DM1 induces maxima of 80% accumulation of cells in G2/M as compared with only 30% in controls in MCF7 cells[2].

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

    分子量

    752.31

    Formula

    C36H50ClN3O10S

    CAS 号

    912569-84-7

    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]. Lopus M, et al. Maytansine and cellular metabolites of antibody-maytansinoid conjugates strongly suppress microtubule dynamics by binding to microtubules. Mol Cancer Ther. 2010 Oct;9(10):2689-99.

      [2]. Oroudjev E, et al. Maytansinoid-antibody conjugates induce mitotic arrest by suppressing microtubule dynamic instability. Mol Cancer Ther. 2010 Oct;9(10):2700-13.

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    DM3-SMe

    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。

    DM3-SMe 

    DM3-SMe 是一种美登素衍生物,是一种微管蛋白 (tubulin) 抑制剂,是一种抗体偶联药物 (ADCs) 的细胞毒性部分,可通过二硫键或稳定的硫醚键与抗体连接。DM3-SMe 在体外显示出高度的细胞毒性活性,IC50 为 0.0011 nM。

    DM3-SMe

    DM3-SMe Chemical Structure

    CAS No. : 796073-70-6

    规格 价格 是否有货
    100 mg ¥41380 询问价格 & 货期

    * Please select Quantity before adding items.

    生物活性

    DM3-SMe is a maytansine derivative and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs), which can be linked to antibody through disulfide bond or stable thioether bond. DM3-SMe shows highly cytotoxic activity in vitro with an IC50 of 0.0011 nM[1][2].

    IC50 & Target[1]

    Maytansinoids

     

    分子量

    812.43

    Formula

    C38H54ClN3O10S2

    CAS 号

    796073-70-6

    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]. Chen H, et al. Tubulin Inhibitor-Based Antibody-Drug Conjugates for Cancer Therapy. Molecules. 2017 Aug 1;22(8).

      [2]. Yuliang Zhaoet al. Biomedical Nanomaterials. 2016-‎Science.

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    DM4-SPDP

    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。

    DM4-SPDP 

    DM4-SPDP 是由 linker SPDP 和 毒性分子 DM4 连接而成的,可用来制备抗体偶联药物。DM4 是抑制细胞分裂的抗微管蛋剂。SPDP 是一种短链交联剂,可通过 NHS-酯和吡啶基二硫醇反应性基团与半胱氨酸巯基形成可降解 (cleavable) 的 (可还原的) 二硫键,实现胺与巯基的结合。

    DM4-SPDP

    DM4-SPDP Chemical Structure

    CAS No. : 2245698-48-8

    规格 价格 是否有货
    1 mg ¥15000 询问价格 & 货期

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    生物活性

    DM4-SPDP is a drug-linker conjugate composed of a potent antitubulin agent DM4 and a linker SMCC to make antibody drug conjugate[1]. SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls[2][3].

    IC50 & Target[1]

    Maytansinoids

     

    分子量

    981.57

    Formula

    C45H61ClN4O14S2

    CAS 号

    2245698-48-8

    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]. Tang R, et al. P-gp activity is a critical resistance factor against AVE9633 and DM4 cytotoxicity in leukaemia cell lines, but not a major mechanism of chemoresistance in cells from acute myeloid leukaemia patients. BMC Cancer. 2009 Jun 23;9:199.

      [2]. Lobedanz S et al. A periplasmic coiled-coil interface underlying TolC recruitment and the assembly of bacterial drug effluxpumps. Proc Natl Acad Sci U S A, 2007 Mar 13, 104(11):4612-7.

      [3]. Karumuthil-Melethil S et al. Dendritic cell-directed CTLA-4 engagement during pancreatic beta cell antigen presentation delays type 1diabetes. J Immunol 2010 Jun 15, 184(12):6695-708.

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    DM3(Synonyms: Maytansinoid DM3)

    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。

    DM3 (Synonyms: Maytansinoid DM3)

    DM3 (Maytansinoid DM3) 是一种带有二硫键或硫醇基的美登素类似物,是一种 tubulin 的抑制剂,还是一种抗体偶联药物 (ADCs) 的细胞毒性部分。

    DM3(Synonyms: Maytansinoid DM3)

    DM3 Chemical Structure

    CAS No. : 796073-54-6

    规格 价格 是否有货
    5 mg ¥7100 询问价格 & 货期
    10 mg ¥12000 询问价格 & 货期

    * Please select Quantity before adding items.

    生物活性

    DM3 (Maytansinoid DM3) is a maytansine analog bearing disulfide or thiol groups and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs)[1].

    IC50 & Target

    Maytansinoids

     

    分子量

    766.34

    Formula

    C37H52ClN3O10S

    CAS 号

    796073-54-6

    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]. Chen H, et al. Tubulin Inhibitor-Based Antibody-Drug Conjugates for Cancer Therapy. Molecules. 2017 Aug 1;22(8).

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    DM4

    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。

    DM4  纯度: 98.80%

    DM4 是抑制细胞分裂的抗微管蛋白剂。DM4 可用于制备抗体药物偶联物。

    DM4

    DM4 Chemical Structure

    CAS No. : 796073-69-3

    规格 价格 是否有货 数量
    10 mM * 1 mL in DMSO ¥1420 In-stock
    5 mg ¥900 In-stock
    10 mg ¥1650 In-stock
    50 mg ¥5500 In-stock
    100 mg   询价  
    200 mg   询价  

    * Please select Quantity before adding items.

    DM4 相关产品

    相关化合物库:

    • Covalent Screening Library Plus
    • Bioactive Compound Library Plus
    • Cell Cycle/DNA Damage Compound Library
    • Toxins for Antibody-Drug Conjugate Research Library
    • Anti-Cancer Compound Library
    • Anti-Aging Compound Library
    • Covalent Screening Library
    • Cytoskeleton Compound Library
    • Anti-Lung Cancer Compound Library

    生物活性

    DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.

    体外研究
    (In Vitro)

    DM4, a structural analogue of maytansine, is a new thiol-containing and potent maytansinoid. DM4 is a cytotoxic maytansinoid drug. It is synthesized in order to link maytansinoids to antibodies via disulfide bonds. Maytansinoids inhibit tubulin polymerization and microtubule assembly and enhance microtubule destabilization, so there is potent suppression of microtubule dynamics resulting in a mitotic block and subsequent apoptotic cell death[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

    780.37

    Formula

    C38H54ClN3O10S

    CAS 号

    796073-69-3

    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 (128.14 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.2814 mL 6.4072 mL 12.8144 mL
    5 mM 0.2563 mL 1.2814 mL 2.5629 mL
    10 mM 0.1281 mL 0.6407 mL 1.2814 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 (3.20 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.20 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 (3.20 mM); Suspended solution; Need ultrasonic

      此方案可获得 2.5 mg/mL (3.20 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 (3.20 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.20 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 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Tang R, et al. P-gp activity is a critical resistance factor against AVE9633 and DM4 cytotoxicity in leukaemia cell lines, but not a major mechanism of chemoresistance in cells from acute myeloid leukaemia patients. BMC Cancer. 2009 Jun 23;9:199.

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    Duocarmycin DM

    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。

    Duocarmycin DM 

    Duocarmycin DM 是一种 DNA 小沟烷基化剂 (DNA minor-groove alkylator),是一种抗体药物结合物 (ADCs) 毒素。Duocarmycin DM 因特有的结构而具有抗癌活性。

    Duocarmycin DM

    Duocarmycin DM Chemical Structure

    规格 是否有货
    5 mg 询价
    10 mg 询价
    25 mg 询价
    50 mg 询价
    100 mg 询价

    * Please select Quantity before adding items.

    生物活性

    Duocarmycin DM, a DNA minor-groove alkylator, is an antibody drug conjugates (ADCs) toxin. Duocarmycin DM is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity[1][2].

    IC50 & Target

    Daunorubicins/Doxorubicins

     

    体外研究
    (In Vitro)

    The Duocarmycins and CC-1065 are members of a class of DNA minor groove, AT-sequence selective, and adenine-N3 alkylating agents, isolated from Streptomyces sp. that exhibit extremely potent cytotoxicity against the growth of cancer cells grown in culture[2].
    Duocarmycin DM shows cytotoxicity to several human cancer cells, with IC50 of 22, 13.8, 3.87, 15.4, and 7.31 pM for HT-29, CL1-5, Caski, EJ, and LS174T, respectively[3].

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

    分子量

    577.98

    Formula

    C28H27ClF3N3O5

    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]. Patil PC, et al. A Short Review on the Synthetic Strategies of Duocarmycin Analogs that are Powerful DNA Alkylating Agents. Anticancer Agents Med Chem. 2015;15(5):616-630.

      [2]. Koch MF, et al. Structural, Biochemical, and Computational Studies Reveal the Mechanism of Selective Aldehyde Dehydrogenase 1A1 Inhibition by Cytotoxic Duocarmycin Analogues. Angew Chem Int Ed Engl. 2015 Nov 9;54(46):13550-4.

      [3]. Chen KC, et al. Selective cancer therapy by extracellular activation of a highly potent glycosidic duocarmycin analogue. Mol Pharm. 2013;10(5):1773-1782.

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    DBCO-PEG4-Ahx-DM1

    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。

    DBCO-PEG4-Ahx-DM1 

    DBCO-PEG4-Ahx-DM1 是由微管蛋白抑制剂 DM1 和连接剂 DBCO-PEG4-Ahx 组成的药物结合剂 (ADC)。Mertansin (DM1) 是一种微管蛋白抑制剂,是一种抗体偶联的美登素毒素,是为了克服与美登素有关的全身毒性和增强肿瘤特异性递送而开发的。

    DBCO-PEG4-Ahx-DM1

    DBCO-PEG4-Ahx-DM1 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

    DBCO-PEG4-Ahx-DM1 is a drug-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody drug conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.

    IC50 & Target

    Maytansinoids

     

    分子量

    1297.92

    Formula

    C68H89ClN6O17

    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.

    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

    SPDB-DM4

    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。

    SPDB-DM4 

    SPDB-DM4 是 ADC 的一部分,由 maytansinebased payload (DM4,一种 tubulin 抑制剂) 和 SPDB 连接而成,具有高效的抗肿瘤活性。

    SPDB-DM4

    SPDB-DM4 Chemical Structure

    CAS No. : 1626359-62-3

    规格 价格 是否有货 数量
    1 mg ¥3500 In-stock
    5 mg ¥9500 In-stock
    10 mg ¥15000 In-stock
    50 mg   询价  
    100 mg   询价  

    * Please select Quantity before adding items.

    生物活性

    SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4, a tubulin inhibitor) via a SPDB linker, exhibiting potent anti-tumor activity.

    IC50 & Target

    Maytansinoids

     

    分子量

    995.59

    Formula

    C46H63ClN4O14S2

    CAS 号

    1626359-62-3

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    -80°C, protect from light, stored under nitrogen

    溶解性数据
    In Vitro: 

    DMSO : 50 mg/mL (50.22 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.0044 mL 5.0221 mL 10.0443 mL
    5 mM 0.2009 mL 1.0044 mL 2.0089 mL
    10 mM 0.1004 mL 0.5022 mL 1.0044 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 (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 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 (2.51 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (2.51 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 (2.51 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (2.51 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
    • 3.

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

      Solubility: ≥ 2.5 mg/mL (2.51 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (2.51 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 上海金畔生物科技有限公司 网站选购。
    参考文献
    • [1]. Puja Sapra, et al. Investigational antibody drug conjugates for solid tumors. Expert Opin Investig Drugs. 2011 Aug;20(8):1131-49.

    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