Orelabrutinib (Synonyms: ICP-022)

Name: Orelabrutinib
Brand: MedChemExpress
SKU: HY-129390
Rating: 5.0 (1 reviews)

Cat. No.: HY-129390 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 1655504-04-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 275	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 275	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 750	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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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

In Vitro

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

MedChemExpress (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].

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

Clinical Trial

Molecular Weight

427.50

Formula

C₂₆H₂₅N₃O₃

CAS No.

1655504-04-3

Appearance

Solid

Color

White to off-white

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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (233.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (271 KB) SDS (252 KB)

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

Handling Instructions (2659 KB)

References

[1]. Wei Xu, et al. Safety, Tolerability and Efficacy of Orelabrutinib, Once a Day, to Treat Chinese Patients with Relapsed or Refractory Chronic Lymphocytic Leukemia/Small Cell Leukemia. Blood (2019) 134 (Supplement_1): 4319.

[2]. BTK Inhibitor ICP-022.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3392 mL	11.6959 mL	23.3918 mL	58.4795 mL
	5 mM	0.4678 mL	2.3392 mL	4.6784 mL	11.6959 mL
	10 mM	0.2339 mL	1.1696 mL	2.3392 mL	5.8480 mL
	15 mM	0.1559 mL	0.7797 mL	1.5595 mL	3.8986 mL
	20 mM	0.1170 mL	0.5848 mL	1.1696 mL	2.9240 mL
	25 mM	0.0936 mL	0.4678 mL	0.9357 mL	2.3392 mL
	30 mM	0.0780 mL	0.3899 mL	0.7797 mL	1.9493 mL
	40 mM	0.0585 mL	0.2924 mL	0.5848 mL	1.4620 mL
	50 mM	0.0468 mL	0.2339 mL	0.4678 mL	1.1696 mL
	60 mM	0.0390 mL	0.1949 mL	0.3899 mL	0.9747 mL
	80 mM	0.0292 mL	0.1462 mL	0.2924 mL	0.7310 mL
	100 mM	0.0234 mL	0.1170 mL	0.2339 mL	0.5848 mL

Orelabrutinib Related Classifications

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.

Keywords:

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

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Orelabrutinib (Synonyms: ICP-022)

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Orelabrutinib Related Antibodies

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Complete Stock Solution Preparation Table

Orelabrutinib Related Classifications

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