2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. Orelabrutinib

Orelabrutinib  (Synonyms: ICP-022)

Cat. No.: HY-129390 Purity: 99.90%
COA Handling Instructions

Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.

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

Orelabrutinib Chemical Structure

Orelabrutinib Chemical Structure

CAS No. : 1655504-04-3

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Solution
10 mM * 1 mL in DMSO USD 275 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Solid
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10 mg USD 400 In-stock
50 mg USD 1200 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK[1][2].

In Vitro

With a proprietary formulation, Orelabrutinib (ICP-022) achieves high bioavailability comparing to other BTK inhibitors[1].

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

Upon administration, Orelabrutinib (ICP-022) binds to and inhibits the activity of BTK. This prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK[2].

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

427.50

Appearance

Solid

Formula

C26H25N3O3
CAS No.
SMILES

O=C(C1=CC=C(C2CCN(C(C=C)=O)CC2)N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)N
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 : 100 mg/mL (233.92 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3392 mL 11.6959 mL 23.3918 mL
5 mM 0.4678 mL 2.3392 mL 4.6784 mL
10 mM 0.2339 mL 1.1696 mL 2.3392 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: ≥ 2.5 mg/mL (5.85 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

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

Purity: 99.90%

COA (246 KB) HNMR (117 KB) RP-HPLC (298 KB) MS (97 KB)

Handling Instructions (2659 KB)
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.

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  • Dilution Calculator

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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

Keywords:

Orelabrutinib1655504-04-3ICP-022ICP022ICP 022BtkBruton tyrosine kinaseMalignancieschroniclymphocytic leukemiasmallBcellantineoplasticInhibitorinhibitorinhibit

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