MedKoo Cat#: 206430 | Name: Belizatinib
Featured New

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

Belizatinib
Belizatinib
CAS#1357920-84-3

Theoretical Analysis

MedKoo Cat#: 206430

Name: Belizatinib

CAS#: 1357920-84-3

Chemical Formula: C33H44FN5O3

Exact Mass: 577.3428

Molecular Weight: 577.75

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 450.00 2 weeks
100mg USD 750.00 2 weeks
200mg USD 1,250.00 2 weeks
500mg USD 1,950.00 2 weeks
1g USD 2,950.00 2 weeks
2g USD 5,450.00 2 weeks
5g USD 7,650.00 2 weeks
Show More
Bulk Inquiry
Buy Now
Add to Cart
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
Solvent mg/mL mM
Solubility
DMF 30.0 51.93
DMSO 143.3 248.08
Ethanol 65.0 112.50
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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
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.