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Qiagen 凯杰 Biosharp Omega

首页酶、辅酶及抑制剂MCE>

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Dxd 10mg

价:
8000.00
价:
¥8000.00

号:HY-13631D

牌:MCE

账期 货到付款

(预计4-5工作日到货(以MCE官网货期为准))

工作时间

周一至周五:9:00-18:00

咨询电话

0771-3293894

在线咨询

客服 郭恒 蔡玉坤 曾宪飞 技术咨询

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Dxd 是一种有效的 DNA topoisomerase I 抑制剂,IC50 值为 0.31 μM,可用作靶作用于 HER2 的 抗体偶联药物 ADC (DS-8201a) 的有效载荷。

Description

Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).

IC50 & Target[1]

Topoisomerase I

0.31 μM (IC50)

In Vitro

Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a). Dxd is cytotoxic to human cancer cell lines of KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC50s of 1.43 nM-4.07 nM, but the control IgG-ADC (Dxd is the payload) shows no inhibition on the four cell lines (with HER2 expression). DS-8201a (Dxd is the payload) displays significant suppression on the HER2-positive KPL-4, NCI-N87, and SK-BR-3 cell lines, with IC50 values of 26.8, 25.4, and 6.7 ng/mL, respectively, but with no such inhibition on MDA-MB-468 (IC50, >10,000 ng/mL)[1].

In Vivo

DS-8201a (Dxd is the payload, 10 mg/kg, i.v.) shows potent antitumor activity in HER2-positive models with KPL4, JIMT-1, and Capan-1 and in HER2 low-expressing ST565 and ST313 models with HER2 IHC 1+/FISH-negative expression[1].

Solvent & Solubility
In Vitro:  

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0264 mL 10.1321 mL 20.2642 mL
5 mM 0.4053 mL 2.0264 mL 4.0528 mL
10 mM 0.2026 mL 1.0132 mL 2.0264 mL
* Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Cells are seeded to a 96-well plate at 1,000 cells per well. After overnight incubation, Dxd is added. Cell viability is evaluated after 6 days using a CellTiter-Glo Luminescent Cell Viability Assay. For the detection of HER2 expression in each cell line, cells are incubated on ice for 30 minutes with FITC Mouse IgG1, κ Isotype Control, or anti-HER2/neu FITC. After washing, the labeled cells are analyzed by FACSCalibur. Relative mean fluorescence intensity (rMFI) is calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Briefly, each cell suspension or tumor fragment is inoculated subcutaneously into specific pathogen-free female nude mice. When the tumor has grown to an appropriate volume, the tumor-bearing mice are randomized into treatment and control groups based on the tumor volumes, and dosing is initiated on day 0. Each substance (DS-8201a, 1 or 10 mg/kg, i.v.; Dxd is the payload) is administered intravenously to the mice. Tumor growth inhibition (TGI, %) is calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

493.48

Formula

C₂₆H₂₄FN₃O₆

CAS No.

1599440-33-1

SMILES

O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C5C6=C(CC[C@@H]5NC(CO)=O)C(C)=C(F)C=C6N=C4C3=C2)=O

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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