2. Vitamin D Related/Nuclear Receptor PROTAC
  3. Androgen Receptor PROTACs
  4. AZ'3137

AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker).

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AZ'3137 Chemical Structure

AZ'3137 Chemical Structure

CAS No. : 2960179-55-7

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AZ'3137 Related Antibodies

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Description

AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker)[1].
In Vitro

AZ'3137 (Compound 22) can inhibit AR signaling and cell proliferation of prostate cancer cell line LNCaP[1].

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

AZ'3137 Related Antibodies

Cell Proliferation Assay[1].

Cell Line: LNCaP cells
Concentration: 0-10 μM
Incubation Time: 7 days
Result: Inhibited the proliferation of LNCaPs with a GI50 value of 74 nM.
In Vivo

AZ'3137 (Compound 22) inhibits tumor growth in prostate cancer mice[1].

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

Animal Model: Immunocompromised NOD SCID male mice implanted with C4-2 cell subcutaneous tumors[1].
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); once daily
Result: Degraded AR and inhibited tumor growth.
Molecular Weight

801.87

Formula

C43H47F4N7O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC(N2CCN(CC3CCN(C4=CC=C(C5CCN(C6=CC=C(C#N)C(C(F)(F)F)=C6F)CC5)C=C4)CC3)CC2)=CC7=C1C(N(C8CCC(NC8=O)=O)C7)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (62.35 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 1.2471 mL 6.2354 mL 12.4708 mL
5 mM 0.2494 mL 1.2471 mL 2.4942 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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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 1.2471 mL 6.2354 mL 12.4708 mL 31.1771 mL
5 mM 0.2494 mL 1.2471 mL 2.4942 mL 6.2354 mL
10 mM 0.1247 mL 0.6235 mL 1.2471 mL 3.1177 mL
15 mM 0.0831 mL 0.4157 mL 0.8314 mL 2.0785 mL
20 mM 0.0624 mL 0.3118 mL 0.6235 mL 1.5589 mL
25 mM 0.0499 mL 0.2494 mL 0.4988 mL 1.2471 mL
30 mM 0.0416 mL 0.2078 mL 0.4157 mL 1.0392 mL
40 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7794 mL
50 mM 0.0249 mL 0.1247 mL 0.2494 mL 0.6235 mL
60 mM 0.0208 mL 0.1039 mL 0.2078 mL 0.5196 mL
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AZ'3137 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:

AZ'31372960179-55-7Androgen ReceptorPROTACsandrogenprostatic cancerorally activeInhibitorinhibitorinhibit

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