2. PROTAC Vitamin D Related/Nuclear Receptor
  3. PROTACs Androgen Receptor
  4. GDC-2992

GDC-2992 (Compound 28A) is an orally bioavailable androgen receptor (AR) PROTAC degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study. (Structure Note: Pink: target protein ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189A); Black: linker (HY-169975); E3 ligase ligand +linker (HY-169976A)).

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GDC-2992 Chemical Structure

GDC-2992 Chemical Structure

CAS No. : 2753651-10-2

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Based on 1 publication(s) in Google Scholar

Other Forms of GDC-2992:

GDC-2992 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

GDC-2992 (Compound 28A) is an orally bioavailable androgen receptor (AR) PROTAC degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study. (Structure Note: Pink: target protein ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189A); Black: linker (HY-169975); E3 ligase ligand +linker (HY-169976A))[1].

In Vitro

GDC-2992 (RO7656594) inhibits AR signaling by binding to both AR and the E3 ubiquitin ligase cereblon (CRBN), resulting in ubiquitination and subsequent degradation of AR[2].
GDC-2992 inhibits AR signaling in the context of wild-type AR and AR proteins with mutations associated with resistance to standard-of-care AR signaling inhibitors (ARSIs)[2].

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

GDC-2992 Related Antibodies
Parmacokinetics
Species Dose Route Indicator value
Dog 10 mg/kg p.o. T1/2 34.3 hr
Rat 10 mg/kg p.o. T1/2 8.28 hr
Dog 10 mg/kg p.o. Cmax 868 ng/mL
Rat 10 mg/kg p.o. Cmax 173 ng/mL
Dog 10 mg/kg p.o. AUC0-inf 15420 ng·h/mL
Rat 10 mg/kg p.o. AUC0-inf 3212 ng·h/mL
Dog 10 mg/kg p.o. F 33.9 %
Rat 10 mg/kg p.o. F 5.13 %
In Vivo

In vivo, GDC-2992 decreases circulating PSA and inhibits prostate tumor growth in a dose responsive manner[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

819.39

Formula

C45H51ClN8O5
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

N#CC1=CC=C(O[C@H]2C(C)(C)[C@H](NC(C3=CC=C(N4CCC(CN5CCN(C6=CC(C=NN([C@@H]7C(NC(CC7)=O)=O)C8=O)=C8C=C6)CC5)CC4)C=C3)=O)C2(C)C)C=C1Cl
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 (61.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2204 mL 6.1021 mL 12.2042 mL
5 mM 0.2441 mL 1.2204 mL 2.4408 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2204 mL 6.1021 mL 12.2042 mL 30.5105 mL
5 mM 0.2441 mL 1.2204 mL 2.4408 mL 6.1021 mL
10 mM 0.1220 mL 0.6102 mL 1.2204 mL 3.0511 mL
15 mM 0.0814 mL 0.4068 mL 0.8136 mL 2.0340 mL
20 mM 0.0610 mL 0.3051 mL 0.6102 mL 1.5255 mL
25 mM 0.0488 mL 0.2441 mL 0.4882 mL 1.2204 mL
30 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.0170 mL
40 mM 0.0305 mL 0.1526 mL 0.3051 mL 0.7628 mL
50 mM 0.0244 mL 0.1220 mL 0.2441 mL 0.6102 mL
60 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5085 mL
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GDC-2992 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GDC-29922753651-10-2RO7656594GDC2992GDC 2992RO 7656594RO-7656594PROTACsAndrogen ReceptorPCaprostaticPROTACdegraderInhibitorinhibitorinhibit

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