GDC-0152
- Product Name
- GDC-0152
- CAS No.
- 873652-48-3
- Chemical Name
- GDC-0152
- Synonyms
- CS-2247;GDC-0152;GDC-0152 ，S7010;GDC0152;GDC 0152.;GDC-0152 (RG7419);GDC-0152 USP/EP/BP;GDC-0152, 10 mM in DMSO;GDC-0152; GDC0152; GDC 0152.;GDC-0152,IAP,Inhibitor,inhibit,GDC 0152;L-Prolinamide, N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-N-(4-phenyl-1,2,3-thiadiazol-5-yl)-
- CBNumber
- CB32665154
- Molecular Formula
- C25H34N6O3S
- Formula Weight
- 498.64
- MOL File
- 873652-48-3.mol
GDC-0152 Property
- Melting point:
- 175-177oC
- storage temp.
- -20°C Freezer
- solubility
- DMSO (Slightly)
- form
- Solid
- color
- White
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 17810
- Product name
- GDC-0152
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 17810
- Product name
- GDC-0152
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $183
- Updated
- 2024/03/01
- Product number
- 17810
- Product name
- GDC-0152
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $299
- Updated
- 2024/03/01
- Product number
- G299920
- Product name
- GDC0152
- Packaging
- 5mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- A4224
- Product name
- GDC-0152
- Packaging
- 10mM(in 1mL DMSO)
- Price
- $140
- Updated
- 2021/12/16
GDC-0152 Chemical Properties,Usage,Production
Uses
GDC 0152 is a peptidomimetic small molecule antagonist of inhibitor of apoptosis (IAP) proteins with antitumor activity.
Biological Activity
gdc-0152 is a potent small-molecule antagonist of inhibitor of apoptosis (iap) proteins, including ml-iap, xiap, ciap1 and ciap2, that binds to the bir domain of ml-iap and the bir3 domains of xiap, ciap1 and ciap2 with values of inhibition constant ki of 14 nm, 28 nm, 17 nm and 43 nm respectively. gdc-0152 potentially inhibits tumor growth of breast cancer by promoting ciap1 degradation and inducing caspase-3/7 activation which result in the decreasing of cell viability of breast cancer cells with normal epithelial cells unaffected. in recent studies, gdc-0152 shows its ability to disrupt the binding of xiap to caspase-9 and the association of ml-iap, ciap1 and ciap2 with smac in hek293t cells.flygare ja, beresini m, budha n, chan h, chan it, cheeti s, cohen f, deshayes k, doerner k, eckhardt sg, elliott lo, feng b, franklin mc, reisner sf, gazzard l, halladay j, hymowitz sg, la h, lorusso p, maurer b, murray l, plise e, quan c, stephan jp, young sg, tom j, tsui v, um j, varfolomeev e, vucic d, wagner aj, wallweber hj, wang l, ware j, wen z, wong h, wong jm, wong m, wong s, yu r, zobel k, fairbrother wj. discovery of a potent small-molecule antagonist of inhibitor of apoptosis (iap) proteins and clinical candidate for the treatment of cancer (gdc-0152). j med chem. 2012;55(9):4101-4113
in vivo
GDC-0152 has moderate predicted hepatic clearance based on metabolic stability assays conducted using human liver microsomes. Plasma?protein binding of GDC-0152 is moderate and comparable among mice (88?91%), rats (89?91%), dogs (81?90%), monkeys (76?85%), and humans (75?83%) over the range of concentrations investigated (0.1?100 μM); higher plasma?protein binding is observed in rabbits (95?96%). GDC-0152 does not preferentially distribute to red blood cells with blood?plasma partition ratios ranging from 0.6 to 1.1 in all species tested. The pharmacokinetics for GDC-0152 is achieved with a C max of 53.7 μM and AUC of 203.5 h·μM[1].
target
XIAP
GDC-0152 Preparation Products And Raw materials
Raw materials
Preparation Products
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