2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. BGB-8035

BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research.

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BGB-8035 Chemical Structure

BGB-8035 Chemical Structure

CAS No. : 2283349-24-4

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Based on 1 publication(s) in Google Scholar

BGB-8035 Related Antibodies

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Description

BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research[1].

IC50 & Target

IC50: 1.1 nM (BTK), 99 nM (TEC), and 621 nM (EGFR)[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
> 10 μM
Compound: (S)-20a; BGB-8035
Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
[PMID: 36912866]
Ramos IC50
> 10 μM
Compound: (S)-20a; BGB-8035
Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
[PMID: 36912866]
Rec1 IC50
10.4 nM
Compound: (S)-20a; BGB-8035
Antiproliferative activity against human REC1 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human REC1 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
[PMID: 36912866]
In Vitro

BGB-8035 is nontoxicin HEK293 and Ramos cells (IC50 > 10 μM, both)[1].

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

BGB-8035 Related Antibodies
In Vivo

BGB-8035 (7.5, 15, 30 mg/kg; PO; twice daily; 16 days) demonstrates dose-dependent antitumor activity[1].
BGB-8035 (1, 3, 10, 30 mg/kg; PO; BID; 13 days) inhibits arthritis as measured by clinical scores in a dose-dependent manner in the Lewis rats aged 8-9 weeks with CIA model and prevents the CIA model-associated body weight loss[1].
Pharmacokinetic Parameters of BGB-8035 in Rats and Dogs[1].

Rats (IV; 1 mg/kg) Rats (PO; 5 mg/kg) Dogs (IV; 1 mg/kg) Dogs (PO; 2.5 mg/kg)
T1/2 (h) 1.0 2.5
CL (mL/min/kg) 24.4 6.89
Vss (L/kg) 0.9 0.74
Tmax (h) 0.25 0.42
Cmax (ng/mL) 667 1246
AUCinf (h∗ng/mL) 964 2645
F (%) 26.4 43

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

Animal Model: Female NOD/SCID mice at 9 weeks of age with REC-1 MCL xenografts[1]
Dosage: 7.5, 15, 30 mg/kg
Administration: PO; BID; 16 days
Result: Demonstrated dose-dependent antitumor activity, with TGI values of 64.1, 73.6, and 79.9%, respectively.
Molecular Weight

453.53

Formula

C24H31N5O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C=CC(N1CCC(CC1)[C@@H]2CCNC3=C(C(C4=CC(OC)=C(C(OC)=C4)C)=NN32)C(N)=O)=O
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 : 50 mg/mL (110.25 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 2.2049 mL 11.0246 mL 22.0493 mL
5 mM 0.4410 mL 2.2049 mL 4.4099 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: 1.25 mg/mL (2.76 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.25 mg/mL (2.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 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 (12.5 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)

g

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
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 2.2049 mL 11.0246 mL 22.0493 mL 55.1231 mL
5 mM 0.4410 mL 2.2049 mL 4.4099 mL 11.0246 mL
10 mM 0.2205 mL 1.1025 mL 2.2049 mL 5.5123 mL
15 mM 0.1470 mL 0.7350 mL 1.4700 mL 3.6749 mL
20 mM 0.1102 mL 0.5512 mL 1.1025 mL 2.7562 mL
25 mM 0.0882 mL 0.4410 mL 0.8820 mL 2.2049 mL
30 mM 0.0735 mL 0.3675 mL 0.7350 mL 1.8374 mL
40 mM 0.0551 mL 0.2756 mL 0.5512 mL 1.3781 mL
50 mM 0.0441 mL 0.2205 mL 0.4410 mL 1.1025 mL
60 mM 0.0367 mL 0.1837 mL 0.3675 mL 0.9187 mL
80 mM 0.0276 mL 0.1378 mL 0.2756 mL 0.6890 mL
100 mM 0.0220 mL 0.1102 mL 0.2205 mL 0.5512 mL
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BGB-8035 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:

BGB-80352283349-24-4BGB8035BGB 8035BtkBruton tyrosine kinaseOrallybruton's tyrosine kinaseTECEGFRantitumorarthritisB-cell malignanciesautoimmuneInhibitorinhibitorinhibit

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