2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Rocbrutinib

Rocbrutinib is an orally available, highly selective Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 of 0.11 nM against wild-type BTK and an IC50 of 1.0 nM against C481S-mutated BTK. Rocbrutinib reduces the viability of leukemia cells, induces cytotoxicity and inhibits cell migration. Rocbrutinib can be used in research related to chronic lymphocytic leukemia, non-Hodgkin's lymphoma and mantle cell lymphoma.

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

Rocbrutinib

Rocbrutinib Chemical Structure

CAS No. : 2485861-07-0

Size Price Stock Quantity
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Rocbrutinib Related Antibodies

Top Publications Citing Use of Products

View All EGFR Isoform Specific Products:

View All Isoforms
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Rocbrutinib is an orally available, highly selective Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 of 0.11 nM against wild-type BTK and an IC50 of 1.0 nM against C481S-mutated BTK. Rocbrutinib reduces the viability of leukemia cells, induces cytotoxicity and inhibits cell migration. Rocbrutinib can be used in research related to chronic lymphocytic leukemia, non-Hodgkin's lymphoma and mantle cell lymphoma[1][2].

In Vitro

Rocbrutinib (LP-168) is a highly selective BTK inhibitor with nanomolar enzymatic potency against both wild-type and BTKC481S[1].
Rocbrutinib (LP-168) (increasing concentrations; 2 hours) inhibits BCR signaling in primary CLL B cells, reducing phosphorylation of BTK and PLCγ2 significantly[1].
Rocbrutinib (LP-168) (2 hours) reduces the migration capacity of primary CLL B cells towards CXCL12 and CXCL14 by over 50%[1].
Rocbrutinib (LP-168) (48 hours) induces dose-dependent cytotoxicity in primary CLL B cells, both in the absence and presence of HS-5 stromal cell support[1].
Rocbrutinib (LP-168) reduces CCL3 and CCL4 chemokine production by primary CLL B cells by 93% each[1].
Rocbrutinib (LP-168) (1 μM) induces modest cytotoxicity and marked reduction of CCL3 and CCL4 production in TMD8 cells expressing BTKT474I[1].
Rocbrutinib (LP-168) induces cytotoxicity and marked reduction of CCL3 and CCL4 production in TMD8 cells expressing BTKC481S[1].
Rocbrutinib forms a covalent bond to BTK's C481 residue and engages in hydrogen bonding with M477, D539, and K430 within the ATP-binding site[2].
Rocbrutinib binds WT BTK (IC50 = 4.7 nM), C481S BTK (IC50 = 49.7 nM), T474I BTK (IC50 = 13.1 nM), and L528W BTK (IC50 = 80.4 nM) with low nanomolar affinity in a NanoBRET assay[2].
Rocbrutinib exhibits nanomolar binding potency to full-length WT BTK and BTK with BTKC481S, BTKV416L, BTKM437R, or BTKL528W mutations in HEK293T cells in an FPCBA[2].
Rocbrutinib inhibits viability of TMD8 cells expressing WT, C481S, T474I, or L528W BTK with nanomolar GI50 potency[2].
Rocbrutinib potently inhibits BCR signaling in TMD8 cells expressing WT, C481S, T474I, or L528W BTK, reducing CCL3/CCL4 cytokine production by >96% and blocking phosphorylation of BTK, PLCγ2, ERK, and AKT[2].
Rocbrutinib (500 nM; 2 hours) inhibits BCR signaling in primary CLL B-cells (including those with BTKC481S), reducing phosphorylation of BTK by 98.9%, PLCγ2 by 85.6%, ERK by 59.3%, and AKT by 68.9%[2].

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

Rocbrutinib Related Antibodies
In Vivo

Rocbrutinib (50 mg/kg; p.o.; daily) significantly improves median survival to 51 days in Eμ-TCL1 chronic lymphocytic leukemia engrafted mice[2].
Rocbrutinib (50 mg/kg; p.o.; daily) significantly improves median survival to 122 days in Eμ-MTCP1 chronic lymphocytic leukemia engrafted mice[2].

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

Animal Model: Eμ-TCL1 (engrafted with chronic lymphocytic leukemia)[2]
Dosage: 50 mg/kg
Administration: p.o.; daily
Result: Extended median survival to 51 days, which was significantly improved relative to vehicle and ibrutinib controls.
Animal Model: Eμ-MTCP1 (engrafted with chronic lymphocytic leukemia)[2]
Dosage: 50 mg/kg
Administration: p.o.; daily
Result: Extended median survival to 122 days, which was significantly improved relative to vehicle and ibrutinib controls.
Molecular Weight

761.91

Formula

C42H51N9O5
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1C2=CC(CC(C)(C3)C)=C3N2CCN1C4=C(C(C(N=C5NC6=CC(NC(C=C)=O)=C(N7[C@H](CN(C8CCOCC8)CC7)C)C=C6)=CN(C)C5=O)=CC=N4)CO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (164.06 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 1.3125 mL 6.5625 mL 13.1249 mL
5 mM 0.2625 mL 1.3125 mL 2.6250 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3125 mL 6.5625 mL 13.1249 mL 32.8123 mL
5 mM 0.2625 mL 1.3125 mL 2.6250 mL 6.5625 mL
10 mM 0.1312 mL 0.6562 mL 1.3125 mL 3.2812 mL
15 mM 0.0875 mL 0.4375 mL 0.8750 mL 2.1875 mL
20 mM 0.0656 mL 0.3281 mL 0.6562 mL 1.6406 mL
25 mM 0.0525 mL 0.2625 mL 0.5250 mL 1.3125 mL
30 mM 0.0437 mL 0.2187 mL 0.4375 mL 1.0937 mL
40 mM 0.0328 mL 0.1641 mL 0.3281 mL 0.8203 mL
50 mM 0.0262 mL 0.1312 mL 0.2625 mL 0.6562 mL
60 mM 0.0219 mL 0.1094 mL 0.2187 mL 0.5469 mL
80 mM 0.0164 mL 0.0820 mL 0.1641 mL 0.4102 mL
100 mM 0.0131 mL 0.0656 mL 0.1312 mL 0.3281 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Rocbrutinib 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:

Rocbrutinib2485861-07-0LP-168LP168LP 168EGFREpidermal growth factor receptorErbB-1HER1AKTmantle cell lymphomaPLCγ2ERKBCR signalingleukemia cellsBruton’s tyrosine kinaseC481S mutant BTKBTKchronic lymphocytic leukemiaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Rocbrutinib
Cat. No.:
HY-156640
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Korean - KR (251 KB) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.