ELMO2-IN-1
ELMO2-IN-1 is an ELMO2 inhibitor with a human target Kd of 1.0 µM. ELMO2-IN-1 binds to ELMO2, disrupting its function. ELMO2-IN-1 induces autophagy-dependent cell death. ELMO2-IN-1 can be used for the research of non-small cell lung cancer.
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- No. CAS: 1216514-48-5
- Fòrmula: C29H28N4O2
- Peso molecular:464.56
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Actividad biológica
ELMO2-IN-1 (Compound C52) (200 μM) binds specifically to wild-type ELMO2 with a Kd of 1.05 μM, and the HIS-435 residue is essential for this binding[1].
ELMO2-IN-1 (72 h) selectively suppresses viability of mesenchymal-like NSCLC cell lines including NCI-H1299, A549, NCI-H1703, 95D, and NCI-H1792 in a concentration-dependent manner, has no effect on normal lung cell lines HBE and MRC-5, and its activity depends on ELMO2 binding and ELMO3 expression levels[1].
ELMO2-IN-1 (5-10 μM; 6-24 h) suppresses FAKY397 phosphorylation in a concentration and time-dependent manner, and induces autophagy markers (reduced p62, increased LC3-II/LC3-I ratio) in mesenchymal-like NSCLC cell lines NCI-H1299 and A549[1].
ELMO2-IN-1 induces cell death in mesenchymal-like patient-derived NSCLC organoids with low ELMO3 expression, but not in epithelial-like organoids with high ELMO3 expression[1].
ELMO2-IN-1 (72 h) potently reduces viability of Osimertinib-resistant NSCLC cell lines NCI-H1975-OR (IC50 = 5.88 μM) and HCC827-OR (IC50 = 7.63 μM), and induces autophagy-related changes in these resistant cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mesenchymal-like NSCLC cell lines (NCI-H1299, A549)
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Concentration:5 μM; 10 μM
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Incubation Time:6 h; 12 h; 24 h
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Result:Suppressed FAK phosphorylation at the Y397 site in a concentration-dependent and time-dependent manner.
Reduced p62 protein expression.
Increased the LC3-II/LC3-I ratio, consistent with induction of autophagy.
ELMO2-IN-1 (25 mg/kg; i.p.; daily for 30 days) does not inhibit the growth of epithelial-like PC-9 non-small cell lung cancer xenografts in female BALB/c nude mice[1].
ELMO2-IN-1 (25 mg/kg; i.p.; daily for 30 days) completely inhibits the growth of Osimertinib (HY-15772)-resistant NCI-H1975-OR non-small cell lung cancer xenografts in female BALB/c nude mice, with no activity against parental NCI-H1975 tumors[1].
ELMO2-IN-1 (25 mg/kg; i.p.; daily for 30 days) does not inhibit the growth of A549 non-small cell lung cancer xenografts expressing ELMO2H435A mutant[1].
ELMO2-IN-1 (2.5-25 mg/kg; i.p.; daily) induces a dose-dependent antitumor response in mesenchymal-like A549 non-small cell lung cancer xenografts in female BALB/c nude mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of mesenchymal-like A549 cells)[1]
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Dosage:25 mg/kg
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Administration:i.p.; daily for 30 days
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Result:Achieved near-complete suppression of tumor growth.
By day 40, mean tumor volume remained near baseline, while vehicle-treated mice had a mean tumor volume of ~1600 mm3 (P<0.0001).
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Animal Model:BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of epithelial-like PC-9 cells)[1]
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Dosage:25 mg/kg
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Administration:i.p.; daily for 30 days
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Result:Showed no significant effect on tumor growth.
By day 40, mean tumor volume in treated and vehicle-treated mice was nearly identical (P=0.9973).
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Animal Model:BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of osimertinib-resistant NCI-H1975-OR cells)[1]
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Dosage:25 mg/kg
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Administration:i.p.; daily for 30 days
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Result:Completely suppressed tumor growth.
By day 40, mean tumor volume remained near baseline, while vehicle-treated mice had a mean tumor volume of ~1200 mm3 (P<0.0001).
Showed no effect on tumor growth in parental NCI-H1975 xenografts (P>0.9999).
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Animal Model:BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of A549 cells expressing ELMO2-H435A mutant)[1]
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Dosage:25 mg/kg
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Administration:i.p.; daily for 30 days
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Result:Failed to suppress growth of tumors expressing the ELMO2-H435A mutant, confirming on-target activity via binding to ELMO2's HIS-435 residue.
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Animal Model:BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of A549 cells)[1]
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Dosage:2.5 mg/kg; 10 mg/kg; 25 mg/kg
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Administration:i.p.; daily
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Result:Exhibited a dose-dependent antitumor response in A549 xenografts.
Chemical Information
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No. CAS 1216514-48-5
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Peso molecular 464.56
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Fòrmula C29H28N4O2
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SMILES
CC(NC(CN1C2=C(C3=C1C(N(C=N3)CC4=CC=CC=C4)=O)C=CC=C2)=O)CCC5=CC=CC=C5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ELMO2-IN-1 Related Classifications
HY-183635 Related Classifications
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