1. PROTAC
  2. E3 Ligase Ligand-Linker Conjugates
  3. Cbl-b-IN-2

Cbl-b-IN-2 

Cat. No.: HY-141431
Handling Instructions

Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent.

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

Cbl-b-IN-2 Chemical Structure

Cbl-b-IN-2 Chemical Structure

CAS No. : 2503325-21-9

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Description

Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent[1].

In Vitro

Cbl-b-IN-2 (Example 8) is a Cbl-b inhibitor with IC50 values range of 5.1-100 nM and ﹤1 nM in high and low concentration of Cbl-b, respectively[1].

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

Cell Viability Assay[1]

Cell Line: Immune cell
Concentration: 0.125 nM, 0.15 nM
Incubation Time: 1 h
Result: Showed Cbl-b activity with an with IC50 values range of 5.1-100 nM and ﹤1 nM in high and low concentration of Cbl-b, respectively.
Molecular Weight

575.57

Appearance

Solid

Formula

C29H30F5N5O2

CAS No.
SMILES

O=C1N(C2=CC=CC(C3(CC4=NN=CN4C)COC3)=C2)CC5=C1C=C(CN6C[[email protected]@H](C)C(F)(F)CC6)C=C5C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 140 mg/mL (243.24 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7374 mL 8.6870 mL 17.3741 mL
5 mM 0.3475 mL 1.7374 mL 3.4748 mL
10 mM 0.1737 mL 0.8687 mL 1.7374 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.5 mg/mL (6.08 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 3.5 mg/mL (6.08 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3.5 mg/mL (6.08 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Product Name:
Cbl-b-IN-2
Cat. No.:
HY-141431
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