1. Protein Tyrosine Kinase/RTK Neuronal Signaling
  2. Anaplastic lymphoma kinase (ALK) Trk Receptor
  3. Belizatinib

Belizatinib  (Synonyms: TSR-011)

Cat. No.: HY-17603 Purity: 99.64%
SDS COA Handling Instructions

Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.

For research use only. We do not sell to patients.

Belizatinib Chemical Structure

Belizatinib Chemical Structure

CAS No. : 1357920-84-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 140 In-stock
Solution
10 mM * 1 mL in DMSO USD 140 In-stock
Solid
2 mg USD 66 In-stock
5 mg USD 110 In-stock
10 mg USD 176 In-stock
25 mg USD 352 In-stock
50 mg USD 495 In-stock
100 mg USD 671 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Belizatinib

View All Trk Receptor Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.

IC50 & Target

IC50: 0.7 nM (ALK)[1]

Cellular Effect
Cell Line Type Value Description References
CHO IC50
231 nM
Compound: 36
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
[PMID: 22734674]
In Vitro

TSR-011 has antitumour activity in the clinical trials.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TSR-011 exerts sustained potent inhibition of ALK-dependent tumour growth in mouse models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

577.73

Formula

C33H44FN5O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 300 mg/mL (519.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7309 mL 8.6546 mL 17.3091 mL
5 mM 0.3462 mL 1.7309 mL 3.4618 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Volume (start)

V1

=
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C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.64%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7309 mL 8.6546 mL 17.3091 mL 43.2728 mL
5 mM 0.3462 mL 1.7309 mL 3.4618 mL 8.6546 mL
10 mM 0.1731 mL 0.8655 mL 1.7309 mL 4.3273 mL
15 mM 0.1154 mL 0.5770 mL 1.1539 mL 2.8849 mL
20 mM 0.0865 mL 0.4327 mL 0.8655 mL 2.1636 mL
25 mM 0.0692 mL 0.3462 mL 0.6924 mL 1.7309 mL
30 mM 0.0577 mL 0.2885 mL 0.5770 mL 1.4424 mL
40 mM 0.0433 mL 0.2164 mL 0.4327 mL 1.0818 mL
50 mM 0.0346 mL 0.1731 mL 0.3462 mL 0.8655 mL
60 mM 0.0288 mL 0.1442 mL 0.2885 mL 0.7212 mL
80 mM 0.0216 mL 0.1082 mL 0.2164 mL 0.5409 mL
100 mM 0.0173 mL 0.0865 mL 0.1731 mL 0.4327 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Belizatinib
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HY-17603
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