Art. -Nr.: HY-149051

BGB-8035

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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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Reinheit: 99.00%
CAS. Nr.: 2283349-24-4
Formel: C₂₄H₃₁N₅O₄
Molecular Weight:453.53

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

BGB-8035 Chemical Structure

CAS. Nr.: 2283349-24-4

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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)
T_1/2 (h)	1.0		2.5
CL (mL/min/kg)	24.4		6.89
V_ss (L/kg)	0.9		0.74
T_max (h)		0.25		0.42
C_max (ng/mL)		667		1246
AUC_inf (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.

Chemical Information

CAS. Nr. 2283349-24-4
Appearance Solid
Molecular Weight 453.53
Formel C₂₄H₃₁N₅O₄
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2049 mL

11.0246 mL

22.0493 mL

5 mM

0.4410 mL

2.2049 mL

4.4099 mL

10 mM

0.2205 mL

1.1025 mL

2.2049 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (251 KB)
- 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yunhang Guo, et al. Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases. J Med Chem. 2023 Mar 23;66(6):4025-4044. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BGB-8035 Related Classifications

HY-149051 Related Classifications