GDC-0917 | CUDC427 | CAS#1446182-94-0 | IAP inhibitor

MedKoo Cat#: 205468 | Name: GDC-0917

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

CUDC-427, also known as, GDC-0917, is an orally available, monovalent mimetic of second mitochondrial-derived activator of caspases (Smac/DIABLO) and inhibitor of IAPs (Inhibitor of Apoptosis Proteins) with potential antineoplastic activity. Smac mimetic CUDC-427 binds to the Smac binding groove on IAPs, including the direct caspase inhibitor X chromosome-linked IAP (XIAP) and the cellular IAPs 1 and 2. This inhibits the activities of these IAPs and promotes the induction of apoptosis through apoptotic signaling pathways.

Chemical Structure

GDC-0917

CAS#1446182-94-0

Theoretical Analysis

MedKoo Cat#: 205468

Name: GDC-0917

CAS#: 1446182-94-0

Chemical Formula: C29H36N6O4S

Exact Mass: 564.2519

Molecular Weight: 564.70

Elemental Analysis: C, 61.68; H, 6.43; N, 14.88; O, 11.33; S, 5.68

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 450.00	2 Weeks
10mg	USD 750.00	2 Weeks

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Related CAS #

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Synonym

GDC0917; GDC-0917; GDC 0917; CUDC427; CUDC-427; CUDC 427

IUPAC/Chemical Name

(S)-1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)-N-(2-(oxazol-2-yl)-4-phenylthiazol-5-yl)pyrrolidine-2-carboxamide

InChi Key

HSHPBORBOJIXSQ-HARLFGEKSA-N

InChi Code

InChI=1S/C29H36N6O4S/c1-18(30-2)24(36)32-23(20-12-7-4-8-13-20)29(38)35-16-9-14-21(35)25(37)34-27-22(19-10-5-3-6-11-19)33-28(40-27)26-31-15-17-39-26/h3,5-6,10-11,15,17-18,20-21,23,30H,4,7-9,12-14,16H2,1-2H3,(H,32,36)(H,34,37)/t18-,21-,23-/m0/s1

SMILES Code

O=C([C@H]1N(C([C@H](C2CCCCC2)NC([C@@H](NC)C)=O)=O)CCC1)NC3=C(C4=CC=CC=C4)N=C(C5=NC=CO5)S3

Appearance

white solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

GDC-0917 free base is soluble in DMSO, not water soluble. GDC-0917 TFA salt is water soluble.

Shelf Life

>2 years if stored properly

Drug Formulation

GDC-0917 TFA was used, which is water soluble. GDC-0917 TFA was formulated in PBS.

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

CUDC-427 is currently developed by Curis, Inc , who licensed from Genentech. CUDC-417 is an orally bioavailable small molecule that triggers tumor cell apoptosis by selectively antagonizing IAP proteins. CUDC-427 was designed to mimic the endogenous IAP antagonist, second mitochondria-derived activator of caspases/direct IAP-binding protein (Smac/DIABLO) that is released into the cytoplasm in response to pro-apoptotic stimuli. CUDC-427 has demonstrated single-agent and combination therapy anti-tumor activity in mouse xenograft tumor models when administered orally, and IND-enabling safety studies have shown it to be well tolerated when dosed daily by oral administration, potentially enabling sustained target inhibition. CUDC-427 is currently developed by , who licensed from Genentech. CUDC-417 is an orally bioavailable small molecule that triggers tumor cell apoptosis by selectively antagonizing IAP proteins. CUDC-427 was designed to mimic the endogenous IAP antagonist, second mitochondria-derived activator of caspases/direct IAP-binding protein (Smac/DIABLO) that is released into the cytoplasm in response to pro-apoptotic stimuli. CUDC-427 has demonstrated single-agent and combination therapy anti-tumor activity in mouse xenograft tumor models when administered orally, and IND-enabling safety studies have shown it to be well tolerated when dosed daily by oral administration, potentially enabling sustained target inhibition.

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 564.70 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Wong H, Gould SE, Budha N, Darbonne WC, Kadel EE 3rd, La H, Alicke B, Halladay JS, Erickson R, Portera C, Tolcher AW, Infante JR, Mamounas M, Flygare JA, Hop CE, Fairbrother WJ. Learning and Confirming with Preclinical Studies: Modeling and Simulation in the Discovery of GDC-0917, an IAP Antagonist. Drug Metab Dispos. 2013 41:2104-2113. PubMed PMID: 24041744.