2. PROTAC GPCR/G Protein
  3. PROTACs Adenosine Receptor
  4. AZD9750

AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant ARL702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research.
(Pink: Adenosine Receptor ligand (HY-175653); Blue: Cereblon ligand (HY-175654); Black: linker).

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

AZD9750

AZD9750 Chemical Structure

CAS No. : 3056515-10-4

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Customer Review

Based on 1 publication(s) in Google Scholar

AZD9750 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Adenosine Receptor Isoform Specific Products:

View All Isoforms
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant ARL702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research[1]. (Pink: Adenosine Receptor ligand (HY-175653); Blue: Cereblon ligand (HY-175654); Black: linker).

IC50 & Target

Cereblon

 

In Vitro

AZD9750 (compound 3n) (0.010-0.012 μM; 24 h) potently degrades wild-type ARWT (with a DC50 of 0.010 μM) in LNCaP cells, as well as mutant ARL702H (with a DC50 of 0.012 μM) in LNCaPL702H cells, after 24 h of treatment.
AZD9750 (0.01-1 μM; 24 h) dose-dependently inhibits the expression of AR-regulated genes (PSA and TMPRSS2) in LNCaP cells[1].
AZD9750 (0.001-1 μM; 10 d) inhibits the proliferation of LNCaP cells in a dose-dependent manner, with the strongest effect observed at the concentration of 1 μM[1].
AZD9750 shows no mitochondrial toxicity in HepG2 cells, with an IC50 as high as 85 μM under galactose conditions and no significant cytotoxicity[1].
AZD9750 (1 μM; 24 h) does not induce the degradation of Ikaros or Aiolos in NB4 cells[1].

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

AZD9750 Related Antibodies

Real Time qPCR[1]

Cell Line: LNCaP
Concentration: 0.0001-1 μM
Incubation Time: 24 h
Result: Dose-dependently inhibited mRNA expression of PSA (KLK3) and TMPRSS2, with statistically significant suppression at concentrations ≥0.01 μM.

Cell Proliferation Assay[1]

Cell Line: LNCaP
Concentration: 0.001-1 μM
Incubation Time: 10 days
Result: Dose-dependently inhibited LNCaP cell proliferation, with maximum suppression observed at 1 μM, resulting in ~30% confluence after 10 days compared to ~95% for DMSO-treated cells.

Western Blot Analysis[1]

Cell Line: NB4
Concentration: 1 μM
Incubation Time: 24 h
Result: Did not degrade Ikaros or Aiolos, as protein expression levels remained similar to DMSO-treated controls.
Parmacokinetics
Species Dose Route CL Vss T1/2 Bioavailability
Mice[1] 0.5 mg/kg i.v. 7.8 mL/min/kg 4.3 L/kg 7.6 h /
Mice[1] 1 mg/kg p.o. / / / 47 %
Rat[1] 0.5 mg/kg i.v. 5.3 mL/min/kg 14 L/kg 31 h /
Rat[1] 1 mg/kg p.o. / / / 53 %
Dog[1] 0.5 mg/kg i.v. 0.81 mL/min/kg 16 L/kg 297 h /
Dog[1] 10 mg/kg p.o. / / / 40 %
In Vivo

AZD9750 (3-60 mg/kg; p.o.; daily; 10 days) dose-dependently reduces seminal vesicle weight in male SCID mice[1].
AZD9750 (30 mg/kg; p.o.; daily; 25 days) achieves 85% tumor growth inhibition and an 86% reduction in AR protein levels in the ST1273 prostate cancer PDX model[1].

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

Animal Model: Crl:NU-(NCr)-Foxn1nu mice with Prostate cancer (male, ST1273 prostate cancer PDX model)[1]
Dosage: 30 mg/kg
Administration: p.o.; daily; 25 days
Result: Inhibited tumor growth by 85% relative to vehicle control.
Reduced androgen receptor (AR) protein levels in tumor samples by an average 86% compared to vehicle control.
Molecular Weight

758.35

Formula

C43H48ClN9O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

N#CC1=NNC2=C(N3C[C@H](C4=CC=C(N5CCC(CC5)CN6CCC(C7=CC8=CC=C(N9C(NC(CC9)=O)=O)C=C8N7C)CC6)C=C4)CCC3)C=CC(Cl)=C12
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 : 25 mg/mL (32.97 mM; ultrasonic and warming and heat to 60°C; 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 1.3187 mL 6.5933 mL 13.1865 mL
5 mM 0.2637 mL 1.3187 mL 2.6373 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
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 1.3187 mL 6.5933 mL 13.1865 mL 32.9663 mL
5 mM 0.2637 mL 1.3187 mL 2.6373 mL 6.5933 mL
10 mM 0.1319 mL 0.6593 mL 1.3187 mL 3.2966 mL
15 mM 0.0879 mL 0.4396 mL 0.8791 mL 2.1978 mL
20 mM 0.0659 mL 0.3297 mL 0.6593 mL 1.6483 mL
25 mM 0.0527 mL 0.2637 mL 0.5275 mL 1.3187 mL
30 mM 0.0440 mL 0.2198 mL 0.4396 mL 1.0989 mL
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AZD9750 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:

AZD97503056515-10-4AZD 9750AZD-9750PROTACsAdenosine ReceptorP1 receptorAR signalingST1273 prostate cancer PDX modelcereblonL702H AR resistance mutantLNCaP cellsLNCaP L702H cellsandrogen receptorproteasomeprostate cancermouse prostate cancer xenograft modelInhibitorinhibitorinhibit

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