Gambogic Acid 2752-65-0

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight:

628.75 Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.


Biological Activity


Gambogic Acid is a caged xanthone that is derived from Garcinia hanburyi
and functions as a strong apoptotic inducer in many types of cancer
cells by inhibiting human Bcl-2 family Proteins and activating caspases.
Gambogic Acid also blocks Kir2.1 channels with EC50 of ≤ 100 nM.
Gambogic Acid significantly inhibits human umbilical vein endothelial
cell (HUVEC) proliferation, migration, invasion, tube formation, and
micro-vessel growth at nM concentration.


Gambogic Acid effectively inhibits tumor Angiogenesis and suppressed
tumor growth with low side effects using metronomic chemotherapy with
Gambogic Acid. Gambogic Acid has multiple functional effects including
the induction of Apoptosis, the inhibition of proliferation and the
prevention of cancer metastasis and tumor angiogenesis. In both animal
tumor models and clinical trials, Gambogic Acid efficiently inhibits
tumor growth with minimal side effects, with little toxicity on immune
and hemopoietic systems. Gambogic Acid can produce tissue-specific
proteasome inhibition and tumor-specific toxicity. LD50: Mice 45mg/kg
(i.p.).


Protocol(Only for Reference)


Kinase Assay: [1]

Competitive peptide displacement assay	GST-Bcl-2 or other GST tagged human Bcl-2 family proteins (100 nmol/L) are incubated with Gambogic Acid at various concentrations for 5 min at room temperature in PBS. Then, 5 nmol FITC-Bid BH3 peptide is added and fluorescence polarization is measured after 10min. IC50 determinations are generated by fitting the experimental data using a sigmoidal dose-response nonlinear regression model.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	628.75
Formula	C38H44O8
CAS No.	2752-65-0

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Chemical Name	2-Butenoic acid, 2-methyl-4-[(1R,3aS,5S,11R,14aS)-3a,4,5,7-tetrahydro-8-hydroxy-3,3,11-trimethyl-13-(3-methyl-2-buten-1-yl)-11-(4-methyl-3-penten-1-yl)-7,15-dioxo-1,5-methano-1H,3H,11H-furo[3,4-g]pyrano[3,2-b]xanthen-1-yl]-, (2Z)-

Molarity Calculator
Dilution Calculator
Molecular Weight Calculator

Contact us if you need more details on 2752-65-0. We are ready to answer your questions on packaging, logistics, certification or any Other aspects about Gambogic Acid 2752-65-0、2752-65-0 Gambogic Acid. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : Apoptosis > Bcl-2 Inhibitor