(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
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
Biological Activity
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(E)-Belizatinib Related Classifications
HY-17603A Related Classifications
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