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Qiagen 凯杰 Biosharp Omega

首页酶、辅酶及抑制剂MCE>

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CUDC-427 纯度:99.60% 10mM*1mL in DMSO

价:
2174.00
价:
¥2174.00

号:HY-15835

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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CUDC-427 是一种高效的 IAP 抑制剂,常用于各种癌症的治疗。

Description

CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.

In Vitro

GDC-0917 (0.1 nM-10 μM) induces reduction of cIAP1 levels in PBMCs in a concentration-dependent manner showing greater than 80% inhibition at concentrations greater than 0.1 µM (56.5 ng/mL)[1].

In Vivo

GDC-0917 (0.08-16.3 mg/kg) exhibits antitumor activity in a dose dependent manner in the MDA-MB-231-X1.1 Breast Cancer Xenograft, and GDC-0917 is well tolerated, with all dose groups experiencing a <11% decrease in mean body weight. GDC-0917 has low to moderate clearance in the mouse (12.0 mL/min/kg), rat (27.0 mL/min/kg), and dog (15.3 mL/min/kg), and high clearance in the monkey (67.6 mL/min/kg). Oral bioavailability is lowest in monkeys compared with other species[1].

Solvent & Solubility
In Vitro:  

DMSO : ≥ 61 mg/mL (108.02 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7709 mL 8.8543 mL 17.7085 mL
5 mM 0.3542 mL 1.7709 mL 3.5417 mL
10 mM 0.1771 mL 0.8854 mL 1.7709 mL
* Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Briefly, 10 million MDA-MB-231-X1.1 breast adenocarcinoma cells resuspended in Hank’s balanced salt solution and Matrigel (1:1, v/v) are implanted subcutaneously into the upper right flank of female SCID.bg mice. MDA-MB-231-X1.1 cells are MDA-MB-231 cells that are selected for improved in vivo growth rates. When tumor volumes reach approximately 100-300 mm3, mice are assigned to treatment groups to get a similar mean tumor size for each treatment group. Treatment groups (n=5 per group) are administered once daily oral doses of vehicle (15% hydroxypropyl-β-cyclodextrin, 20 mM succinic acid in water), 0.08, 0.17, 0.34, 0.68, 1.36, 2.72, 5.43, 10.87, or 16.30 mg/kg of GDC-0917 for 21 days. Tumor volumes are measured in two dimensions (length and width) using Ultra Cal IV calipers. Tumor sizes and body weights are recorded twice weekly, and the mice are regularly observed over the course of the study. Mice are euthanized if their tumor volume exceeds 2000 mm3 or if their body weight drops by more than 20% of the starting weight.

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

References
Molecular Weight

564.70

Formula

C₂₉H₃₆N₆O₄S

CAS No.

1446182-94-0

SMILES

O=C([C@H](CCC1)N1C([C@H](C2CCCCC2)NC([C@H](C)NC)=O)=O)NC3=C(C4=CC=CC=C4)N=C(C5=NC=CO5)S3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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