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

Orelabrutinib (Synonyms: ICP-022)

Cat. No.: HY-129390 Purity: 98.93%
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

Size Price Stock Quantity
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
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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].

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].

Molecular Weight

427.50

Formula

C₂₆H₂₅N₃O₃

CAS No.

1655504-04-3

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 : 250 mg/mL (584.80 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: ≥ 6.25 mg/mL (14.62 mM); Clear solution

  • 2.

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

    Solubility: ≥ 6.25 mg/mL (14.62 mM); Clear solution

  • 3.

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

    Solubility: ≥ 6.25 mg/mL (14.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

OrelabrutinibICP-022ICP022ICP 022BtkBruton tyrosine kinaseMalignancieschroniclymphocytic leukemiasmallBcellantineoplasticInhibitorinhibitorinhibit

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Orelabrutinib
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HY-129390
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