eALM1192
eALM1192 is a selective mTOR kinase inhibitor (IC50 = 2.3 nM) that also inhibits DNA-PK (IC50 = 84 nM), PI3Kα, and PKN3, with 37-fold selectivity for mTOR over DNA-PK. eALM1192 exhibits antiproliferative activity against cancer cell lines and colorectal cancer cell lines. eALM1192 can be used for colorectal cancer research.
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- CAS No.: 3134761-90-0
- 화학식: C23H23N7O3
- 분자량:445.47
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
mTOR 2.3 nM (IC50) |
DNA-PK 84 nM (IC50) |
PI3Kα |
PKN3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW48 | EC50 |
5.6 nM
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Antiproliferative activity against human SW48 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
Antiproliferative activity against human SW48 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
|
D6MD00572A |
| HCT-116 | EC50 |
49 nM
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Antiproliferative activity against human HCT116 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
Antiproliferative activity against human HCT116 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
|
D6MD00572A |
| SW480 | EC50 |
63 nM
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Antiproliferative activity against human SW480 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
Antiproliferative activity against human SW480 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
|
D6MD00572A |
In Vitro
2w (eALM1192) (1-10000 nM; 5 days) exhibits potent low-nanomolar antiproliferative activity across SW48, HCT116 and SW480 colorectal cancer cell lines[1].
eALM1192 (1 μM) acts as a highly selective inhibitor, demonstrating potent activity (determined as residual activity at 1 μM) primarily against MTOR, DNAPK, and PIK3CA/PIK3R1.
2w (eALM1192) (0.09-3000 nM) is a potent mTOR inhibitor with an IC50 of 2.3 nM and 37-fold selectivity over DNA-PK[1].
2w (eALM1192) (1 µM; 0-45 min) demonstrates excellent metabolic stability with a half-life of 109 min in human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3134761-90-0
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분자량 445.47
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화학식 C23H23N7O3
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SMILES
O=C(N1CCC(CN2C=C(C3=CC=C(OC(N)=N4)C4=C3)C5=C(N)N=CN=C52)CC1)OCC#C
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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)
eALM1192 Related Classifications
HY-189486 Related Classifications
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