AZ'4331
AZ'4331 is an orally active pan-TEAD family inhibitor, with an IC50 of 0.381 μM against TEAD1, 0.020 μM against TEAD2, 0.014 μM against TEAD3, and 0.031 μM against TEAD4. AZ'4331 slows cell cycle progression. AZ'4331 exerts effects in cancer xenograft models with dysregulated Hippo pathway. AZ'4331 can be used to study cancers with altered Hippo pathways, including mesothelioma, head and neck squamous cell carcinoma, and EGFR-mutant non-small cell lung cancer.
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- CAS No.: 3006101-94-3
- 화학식: C21H18F3N5O
- 분자량:413.40
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Biological Activity
제품 설명
IC50 & Target
[1]|
TEAD1 0.381 μM (IC50) |
TEAD2 0.020 μM (IC50) |
TEAD3 0.014 μM (IC50) |
TEAD4 0.031 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H226 | IC50 |
9.6 nM
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Disruption of YAP-TEAD protein-protein association in NCI-H226 NF2-deleted mesothelioma cells after 24 hours of incubation measured by pre-permeabilization immunofluorescence assay.
Disruption of YAP-TEAD protein-protein association in NCI-H226 NF2-deleted mesothelioma cells after 24 hours of incubation measured by pre-permeabilization immunofluorescence assay.
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42525965 |
| MCF7 | IC50 |
20 nM
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Inhibition of TEAD-dependent luciferase expression in MCF7 TEAD Reporter cells after 24 hours of incubation assessed using Bright-Glo reagent luminescence measurement.
Inhibition of TEAD-dependent luciferase expression in MCF7 TEAD Reporter cells after 24 hours of incubation assessed using Bright-Glo reagent luminescence measurement.
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42525965 |
| NCI-H226 | GI50 |
92 nM
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Inhibition of proliferation of NCI-H226 (NF2-deleted) mesothelioma cells after 72 hours of incubation measured by CellTiter-Glo luminescence assay.
Inhibition of proliferation of NCI-H226 (NF2-deleted) mesothelioma cells after 72 hours of incubation measured by CellTiter-Glo luminescence assay.
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42525965 |
| NCI-H2452 | GI50 |
>18 μM
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Growth inhibition of NCI-H2452 (NF2-wildtype) mesothelioma cells after 72 hours of incubation measured by CellTiter-Glo luminescence assay.
Growth inhibition of NCI-H2452 (NF2-wildtype) mesothelioma cells after 72 hours of incubation measured by CellTiter-Glo luminescence assay.
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42525965 |
| NCI-H226 | IC50 |
29 nM
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Reduction in the fraction of EdU-positive S-phase cells in NCI-H226 NF2-deleted mesothelioma cells after 48 hours of compound incubation followed by 1 hour of 10 µM EdU labeling measured by Click-IT EdU Alexa Fluor 488 HCS Assay and high-content microscopy.
Reduction in the fraction of EdU-positive S-phase cells in NCI-H226 NF2-deleted mesothelioma cells after 48 hours of compound incubation followed by 1 hour of 10 µM EdU labeling measured by Click-IT EdU Alexa Fluor 488 HCS Assay and high-content microscopy.
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42525965 |
In Vitro
AZ'4331 inhibits TEAD1, TEAD2, TEAD3, and TEAD4 with IC50 values of 0.381 μM, 0.020 μM, 0.014 μM, and 0.031 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AZ'4331 (100 mg/kg; p.o.; once daily; 21 days) induces near-complete tumor regression in LATS1/2-deleted MSTO-211H mesothelioma xenografts following 21 days of once-daily 100 mg/kg oral dosing[1].
AZ'4331 (100 mg/kg; p.o.; once daily; 21 days) delivers tumor growth inhibition in FAT1-mutated FaDu HNSCC xenografts following 21 days of once-daily 100 mg/kg oral dosing[1].
AZ'4331 (100 mg/kg; p.o.) modestly suppresses TEAD target gene upregulation in EGFR-mutant NSCLC PDX models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17 SCID mice (Female, CB17/Icr-Prkdcscid/IcrIcoCrl)[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; once daily; 28 days
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Result:Produced exposure-dependent tumor growth inhibition, with the 100 mg/kg dose resulting in a 50% regression from the starting tumor volume.
Showed no significant body weight loss across all dose groups.
Induced exposure-dependent suppression of canonical TEAD target gene CTGF expression in tumors following both a single acute dose and 4 consecutive days of daily dosing.
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Animal Model:CB17 SCID mice (Female, CB17/Icr-Prkdcscid/IcrIcoCrl)[1]
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Dosage:100 mg/kg
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Administration:p.o.; once daily; 21 days
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Result:Resulted in near-complete regression of established MSTO-211H LATS1/2-deleted mesothelioma tumors.
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Animal Model:NCr-Nude mice (Female, CrTac:NCr-Foxn1nu)[1]
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Dosage:100 mg/kg
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Administration:p.o.; once daily; 21 days
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Result:Produced tumor growth inhibition in FaDu HNSCC xenografts.
Chemical Information
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CAS No. 3006101-94-3
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분자량 413.40
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화학식 C21H18F3N5O
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SMILES
C=CC(N(C1)CC[C@@H]1NC2=NC=C(C3=CC=C(C(F)(F)F)C=N3)C4=NC=CC=C42)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AZ'4331 Related Classifications
HY-189200 Related Classifications
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