Belizatinib
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MedKoo CAT#: 206430

CAS#: 1357920-84-3

Description: Belizatinib, also known as TSR-011, is an orally available inhibitor of both the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) and the tropomyosin-related kinases (TRK) TRKA, TRKB, and TRKC, with potential antineoplastic activity. Upon administration, ALK/TRK inhibitor TSR-011 binds to and inhibits both ALK and TRK kinases. The inhibition leads to disruption of ALK- and TRK-mediated signaling and impedes tumor cell growth in ALK/TRK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors.


Chemical Structure

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Belizatinib
CAS# 1357920-84-3

Theoretical Analysis

MedKoo Cat#: 206430
Name: Belizatinib
CAS#: 1357920-84-3
Chemical Formula: C33H44FN5O3
Exact Mass: 577.34
Molecular Weight: 577.750
Elemental Analysis: C, 68.61; H, 7.68; F, 3.29; N, 12.12; O, 8.31

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 weeks
100mg USD 750 2 weeks
200mg USD 1250 2 weeks
500mg USD 1950 2 weeks
1g USD 2950 2 weeks
2g USD 5450 2 weeks
5g USD 7650 2 weeks
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Related CAS #: 1357920-84-3   1388225-79-3 (TSR-011 isomer)    

Synonym: TSR011; TSR011; TSR 011; Belizatinib

IUPAC/Chemical Name: 4-fluoro-N-(6-((4-(2-hydroxypropan-2-yl)piperidin-1-yl)methyl)-1-((1s,4s)-4-(isopropylcarbamoyl)cyclohexyl)-1H-benzo[d]imidazol-2-yl)benzamide

InChi Key: WSTUJEXAPHIEIM-FEGDYQJNSA-N

InChi Code: InChI=1S/C33H44FN5O3/c1-21(2)35-30(40)24-8-12-27(13-9-24)39-29-19-22(20-38-17-15-25(16-18-38)33(3,4)42)5-14-28(29)36-32(39)37-31(41)23-6-10-26(34)11-7-23/h5-7,10-11,14,19,21,24-25,27,42H,8-9,12-13,15-18,20H2,1-4H3,(H,35,40)(H,36,37,41)/t24-,27+

SMILES Code: O=C(NC1=NC2=CC=C(CN3CCC(C(C)(O)C)CC3)C=C2N1[C@H]4CC[C@@H](C(NC(C)C)=O)CC4)C5=CC=C(F)C=C5

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 30.0 51.93
DMSO 143.3 248.08
Ethanol 65.0 112.50

Preparing Stock Solutions

The following data is based on the product molecular weight 577.75 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Attwa MW, Kadi AA, Darwish HW. Belizatinib: Novel reactive intermediates and bioactivation pathways characterized by LC-MS/MS. J Pharm Biomed Anal. 2019 Jul 15;171:132-147. doi: 10.1016/j.jpba.2019.04.006. Epub 2019 Apr 6. PMID: 30999224.


2: Lin CC, Arkenau HT, Lu S, Sachdev J, de Castro Carpeño J, Mita M, Dziadziuszko R, Su WC, Bobilev D, Hughes L, Chan J, Zhang ZY, Weiss GJ. A phase 1, open-label, dose-escalation trial of oral TSR-011 in patients with advanced solid tumours and lymphomas. Br J Cancer. 2019 Jul;121(2):131-138. doi: 10.1038/s41416-019-0503-9. Epub 2019 Jun 20. PMID: 31217479; PMCID: PMC6738096.