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

AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC50 value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC50 of 92 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.
(Pink: Androgen Receptor ligand (HY-172954); Blue: Cereblon ligand (HY-172955); Black: linker (HY-W262798)).

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AZ'3137

AZ'3137 構造式

CAS 番号 : 2960179-55-7

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 662 在庫あり
Solution
10 mM * 1 mL in DMSO USD 662 在庫あり
Solid
5 mg $375 在庫あり
10 mg $600 在庫あり
25 mg $1200 在庫あり
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AZ'3137 関連抗体

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すべてのアイソフォームを表示
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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製品説明

AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC50 value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC50 of 92 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[1]. (Pink: Androgen Receptor ligand (HY-172954); Blue: Cereblon ligand (HY-172955); Black: linker (HY-W262798)).

Cellular Effect
Cell Line Type Value Description References
LNCaP GI50
74 nM
Compound: 22; AZ'3137
Anti-proliferative activity against human LNCaP cells assessed as number of live cells measured after 7 days by Sytox Green Nucleic Acid stain assay
Anti-proliferative activity against human LNCaP cells assessed as number of live cells measured after 7 days by Sytox Green Nucleic Acid stain assay
[PMID: 38991141]
体外実験

AZ'3137 (Compound 22; 0-10 μM; 7 days) can inhibit AR signaling and cell proliferation of prostate cancer cell line LNCaP[1].
AZ′3137 (0.1 nM-10 μM; 24 h) inhibits the expression of AR target genes in LNCaP cells[1].
AZ′3137 (0.1 nM-10 μM; 24 h) is able to degrade AR in C4-2 and VCAP cells[1].

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

AZ'3137 関連抗体

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.

RT-PCR[1].

Cell Line: LNCaP cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM
Incubation Time: 24 h
Result: Was able to inhibit the expression of AR target genes.

Western Blot Analysis[1].

Cell Line: C42 cells and VCAP cells
Concentration: 0.1 nM, 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM
Incubation Time: 24 h
Result: Was able to degrade AR.
体内実験

AZ'3137 (Compound 22; oral gavage (p.o.); once daily; for 10 days) 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; for 10 days
Result: Degraded AR and inhibited tumor growth.
分子量

801.87

分子式

C43H47F4N7O4
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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
10 mM 0.1247 mL 0.6235 mL 1.2471 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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純度とドキュメンテーション
参考文献

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

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質量   濃度   体積   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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'31372960179-55-7PROTACsAndrogen Receptorandrogenprostatic cancerorally activePROTACARInhibitorinhibitorinhibit

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製品名:
AZ'3137
製品番号:
HY-162702
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