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Art. -Nr.: HY-184865

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Anticancer agent 340

Anticancer agent 340 is an orally active antitumor agent. Anticancer agent 340 can bind to both the androgen receptor (AR) and BRD4 protein simultaneously, dose-dependently inducing the formation of the AR-BRD4 ternary complex, inhibiting the expression of the downstream target gene HEXIM1 (Gene X), and activating the Caspase 3/7 pathway to initiate apoptosis. Its proliferation inhibition and apoptosis activities are both significantly AR expression-dependent. Anticancer agent 340 can be used to study AR/BRD4 driven malignancies such as castration-resistant prostate cancer (CRPC).

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CAS. Nr.: 3032493-76-5
Formel: C₄₉H₅₁ClN₁₀O₄S
Molecular Weight:911.51

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Anticancer agent 340 Chemical Structure

CAS. Nr.: 3032493-76-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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In Vitro

Anticancer agent 340 (compound I-49) (0.1 nM-10 μM; 6 days) exhibits potent inhibitory activity against AR-dependent prostate cancer cells , and its antiproliferative activity depends on the expression of full-length AR^[1].
Anticancer agent 340 (serial dilutions; 72 h) exhibits potent inhibitory activity against the proliferation of T-Rex 293 cell line SC cells^[1].
Anticancer agent 340 (serial dilutions; 24-48 h)-induced apoptosis in 22RV1 parental cells depends on the expression level of full-length AR (FL-AR) ^[1].
Anticancer agent 340 (serial dilutions; 16 h) effectively inhibits the expression of downstream target genes of EP (BRD4), validating the target engagement of PROTAC^[1].
Anticancer agent 340 (serial dilutions; 1 h) dose-dependently induces the formation of the AR-compound-EP ternary complex; neither AR ligand alone nor EP ligand alone can induce the formation of the ternary complex^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

LnCaP95 parental cells
Concentration:

0.1 nM-10 μM
Incubation Time:

4 h
Result:

Had a GI₅₀ of 37 nM in LnCaP95 parental cells.

Cell Proliferation Assay^[1]

Cell Line:

T-Rex 293 cell line SC cells
Concentration:

serial dilutions
Incubation Time:

72 h
Result:

Strongly inhibited cell proliferation.

Apoptosis Analysis^[1]

Cell Line:

22RV1 parental cells
Concentration:

serial dilutions
Incubation Time:

24-48 h
Result:

Showed an EC₅₀ of 126 nM in FL-AR-overexpressing 22RV1 cells.
Significantly reduced apoptosis activity in FL-AR-underexpressing cells.

RT-PCR^[1]

Cell Line:

TReX293 cells
Concentration:

serial dilutions
Incubation Time:

16 h
Result:

Dose-dependently reduced Gene X mRNA levels.

In Vivo

Anticancer agent 340 (compound I-49) (10-100 mg/kg; p.o.; once daily) exerts robust antitumor activity in castration-resistant prostate cancer in vivo, reduces the prostate cancer biomarker PSA correspondingly, and validates its PROTAC mechanism by inducing AR/BRD4 ternary complex formation in tumor tissues^[1].
Anticancer agent 340 (10-100 mg/kg; p.o.; once daily; for 3 days) can effectively penetrate tumor tissue in vivo and inhibit the expression of downstream genes of EP (BRD4), demonstrating good PD efficacy^[1].

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

Animal Model:

CB17.SCID immunodeficient mice were subcutaneously implanted with 5×10₆ VCaP cells suspended in 50% Matrigel^[1]
Dosage:

10 mg/kg; 30 mg/kg; 100 mg/kg
Administration:

p.o., once daily
Result:

Dose-dependently inhibited the growth of castrated VCaP tumors.
Dose-dependently reduced plasma PSA concentration.
Dose-dependently induces the formation of the AR-compound-BRD4 ternary complex in tumor tissue.

Animal Model:

CB17.SCID immunodeficient mice were subcutaneously implanted with 5×10₆ VCaP cells suspended in 50% Matrigel^[1]
Dosage:

10 mg/kg; 30 mg/kg; 100 mg/kg
Administration:

p.o., once daily; for 3 days
Result:

Dose-dependently reduced Gene X mRNA levels in tumor tissue.

Chemical Information

CAS. Nr. 3032493-76-5
Molecular Weight 911.51
Formel C₄₉H₅₁ClN₁₀O₄S
SMILES

CC(C)([C@H](C1(C)C)OC2=CC(Cl)=C(C=C2)C#N)[C@H]1NC(C3=CN=C(N=C3)N(CC4)CCC4(C5)CC5OC6=CC=C(C7=N[C@@H](CC8=NC=CO8)C9=NN=C(C)N9C%10=C7C(C)=C(C)S%10)C=C6)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Eastman KL, et al.; Halda Therapeutics Opco Inc., assignee. Synthetic RIPTAC AR and BRD4 dual degraders for castration-resistant prostate cancer. WO2024054603 A1. PCT International Application No. PCT/US2023/032252, filed 2023 Sep 8, published 2024 Mar 14.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
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- In Vivo
Chemical Information
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Anticancer agent 340

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