(E)-Belizatinib
(E)-Belizatinib ((E)-TSR-011)) (compound 36), the (E)-isomer of Belizatinib (HY-17603), is a potent, selective and orally active anaplastic lymphoma kinase (ALK) Inhibitor with an enzymatic IC50 of 0.005 μM and a cellular IC50 of 0.048 μM. (E)-Belizatinib shows >61-fold selectivity over JAK2, SRC, and IGF1R. (E)-Belizatinib shows favorable potency and PK characteristics in rats and dogs. (E)-Belizatinib can be used for ALK-driven cancer research.
For research use only. We do not sell to patients.
- CAS No.: 1388225-72-6
- Formula: C33H44FN5O3
- Molecular Weight:577.73
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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
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
231 nM
Compound: 36
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Inhibition of INSR expressed in CHO cells assessed as inhibition of receptor phosphorylation pre-incubated before insulin stimulation by Meso-Scale Discovery pY-IR assay
Inhibition of INSR expressed in CHO cells assessed as inhibition of receptor phosphorylation pre-incubated before insulin stimulation by Meso-Scale Discovery pY-IR assay
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[PMID: 22734674] |
Chemical Information
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CAS No. 1388225-72-6
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Molecular Weight 577.73
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Formula C33H44FN5O3
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SMILES
O=C(C1=CC=C(C=C1)F)NC(N([C@H]2CC[C@H](CC2)C(NC(C)C)=O)C3=C4)=NC3=CC=C4CN5CCC(CC5)C(C)(O)C
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Synonyms
(E)-TSR-011
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(E)-Belizatinib Related Classifications
HY-17603A Related Classifications
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