PROTAC EML4-ALK Degrader-1
PROTAC EML4-ALK Degrader-2 (Pro-BA) is a selective and orally active linker-free EML4-ALK PROTAC degrader with the DC50 of 74 nM in H1322 cells (T1/2 = 8 h). PROTAC EML4-ALK Degrader-2 relies on GID4 and proteasome pathways to promote ubiquitination of target proteins, leading to cell apoptosis. PROTAC EML4-ALK Degrader-2 can be used for research on cancer.
(Pink: EML4-ALK ligand (HY-150908); Blue: GID4 ligand (HY-40114); Black: linker).
For research use only. We do not sell to patients.
- Formula: C28H35ClN7O3P
- Molecular Weight:584.05
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
PROTAC EML4-ALK Degrader-2 (Compound Pro-BA) (0-1 μM; 0-24 h) can significantly and selectively degrade the levels of EML4-ALK in H3122 (DC50 = 74 nM), BaF3-EML4-ALK (DC50 = 125 nM) and neuroblastoma SK-N-BE(2) cells (DC50 = 2.1 μM)[1].
PROTAC EML4-ALK Degrader-2 (500 nM; 24 h) increases the proportion of G1 phase cells and significantly increases cell apoptosis in H3122 cells[1].
PROTAC EML4-ALK Degrader-2 (500 nM; 24 h) induces the degradation of EML4-ALK through the ubiquitin-proteasome system in HEK293T cells.[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H3122 cells
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Concentration:500 nM
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Incubation Time:24 h
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Result:Increased the proportion of G1 phase cells.
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Cell Line:H3122 cells
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Concentration:0-1 μM
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Incubation Time:48 h
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Result:Significantly inhibited the growth of H3122 cells (IC50 = 34 nM).
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Cell Line:H3122 cells
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Concentration:500 nM
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Incubation Time:24 h
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Result:Significantly increased the proportion of early and late apoptosis.
PROTAC EML4-ALK Degrader-2 (25 mg/kg; p.o.; every two days; a total of 8 doses) reduces the level of EML4-ALK and inhibits tumor growth, and exhibits low toxicity in the female nude mice with H3122 xenograft tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:1×107 H3122 cells injected female nude mice (4 weeks)[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection (i.p.); every other day for a total of 8 doses
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Result:Significantly reduced the level of EML4-ALK protein in tumors.
Had good tolerance and no significant change in weight.
Significantly inhibits the volume of tumors.
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Animal Model:1×107 H3122 cells injected female nude mice (4 weeks)[1]
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Dosage:25 mg/kg
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Administration:Oral administration (p.o.); every two days for a total of 8 doses
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Result:Significantly reduced the level of EML4-ALK protein in tumors.
Significantly inhibits the volume of tumors.
Did not change the structure in the main organs.
Chemical Information
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Molecular Weight 584.05
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Formula C28H35ClN7O3P
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SMILES
COC1=C(C=CC(N2CCN(CC2)C([C@H]3CCCN3)=O)=C1)NC4=NC=C(C(NC5=CC=CC=C5P(C)(C)=O)=N4)Cl
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Synonyms
Pro-BA
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC EML4-ALK Degrader-1 Related Classifications
HY-174368 Related Classifications
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