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Berbamine dihydrochloride Bcr-Abl inhibitor

Name: Berbamine dihydrochloride
Brand: Selleck Chemicals
SKU: S3609
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S3609

Berbamine (BA, BBM) dihydrochloride, a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA, BBM) dihydrochloride induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII).

Chemical Structure

Molecular Weight: 681.65

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Quality Control

Batch: Purity: 99.72%

99.72

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2
Other Bcr-Abl Inhibitors	Degrasyn (WP1130) Bafetinib Rebastinib (DCC-2036) GNF-5 Berbamine GNF-2 GNF-7 Olverembatinib (GZD824) dimesylate PD173955 Radotinib

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (146.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 50 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	681.65	Formula	C₃₇H₄₀N₂O₆.2HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	6078-17-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BA, BBM			Smiles	CN1CCC2=CC(=C3C=C2C1CC4=CC=C(C=C4)OC5=C(C=CC(=C5)CC6C7=C(O3)C(=C(C=C7CCN6C)OC)OC)O)OC.Cl

Mechanism of Action

Targets/IC₅₀/Ki	Bcr-Abl NF-κB CaMKII
In vitro	Berbamine (BBM) potently suppresses liver cancer cell proliferation and induces cancer cell death by targeting Ca2+/calmodulin-dependent protein kinase II (CAMKII). Through targeting CAMKII, BBM's inhibition on cancer cells might have broader effects beyond affecting JAK/STAT3 and p210bcr-abl, because CAMKIIγ directly impacts many other signal pathways including STAT1, NF-κB, JNK, ERK1/2, FOXO1, and Wnt/β-catenin. BBM can effectively inhibit tumor metastasis by suppressing cell proliferation, migration and invasion in highly metastatic breast cancer cells under in vitro condition. Berbamine inhibits proliferation of K562-r cells both in vitro and in vivo. Berbamine-induced apoptosis in K562-r cells appear to occur through a mechanism involving Bcl-2 family proteins, as well as mdr-1 mRNA and P-gp protein. Berbamine in combination restore the chemo-sensitivity of K562-r cells.
In vivo	BBM inhibits the in vivo tumorigenicity of liver cancer cells in NOD/SCID mice, and down-regulated the self-renewal abilities of liver cancer initiating cells. BBM shows its anticancer activity by induction of apoptosis, cell cycle arrest and reversing multidrug resistance. Though BBM is a potent drug but its half-life in blood plasma is very short, owing to its quick renal clearance.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23960096/ [2] https://www.nature.com/articles/s41598-017-05296-y [3] https://pubmed.ncbi.nlm.nih.gov/19270722/ [4] https://pubmed.ncbi.nlm.nih.gov/16023722/ [5] https://pubmed.ncbi.nlm.nih.gov/19960011/

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