1. Apoptosis
  2. IAP

CUDC-427 (Synonyms: GDC-0917)

Cat. No.: HY-15835 Purity: 99.60%
Data Sheet SDS Handling Instructions

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

For research use only. We do not sell to patients.
CUDC-427 Chemical Structure

CUDC-427 Chemical Structure

CAS No. : 1446182-94-0

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $217 In-stock
5 mg $175 In-stock
10 mg $275 In-stock
50 mg $750 In-stock
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200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

References
Preparing Stock Solutions
Concentration Volume 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.
Animal Administration
[1]

CUDC-427 is formulated in 15% hydroxypropyl-β-cyclodextrin, 20 mM succinic acid in water.

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. The following formula is used with Excel version 11.2 to calculate tumor volume (TV): TV (mm3) = (Length × Width2) ×0.5. 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

564.7

Formula

C₂₉H₃₆N₆O₄S

CAS No.

1446182-94-0

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

Solvent & Solubility

DMSO: ≥ 61 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
CUDC-427
Cat. No.:
HY-15835
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