[CAS NO. 1446182-94-0]  CUDC-427

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PRODUCTS SPECIFICATIONS [1446182-94-0]

Catalog
HY-15835
Brand
MCE
CAS
1446182-94-0

DESCRIPTION [1446182-94-0]

Overview

MDL-
Molecular Weight564.70
Molecular FormulaC29H36N6O4S
SMILESO=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

For research use only. We do not sell to patients.


Summary

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] .

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


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] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT01226277 Genentech, Inc.
Solid Cancers
October 2010 Phase 1
NCT01908413 Curis, Inc.
Lymphoma
July 2013 Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

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

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 88.54 mM ; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution

* All of the co-solvents are available by MCE.