research use only

Betulinic acid Topoisomerase inhibitor

Name: Betulinic acid
Brand: Selleck Chemicals
SKU: S3603
Availability: InStock
Rating: 5 (15 reviews)

Cat.No.S3603

Betulinic acid (ALS-357, Lupatic acid, Betulic acid), a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. It's reported that this compound acts as a new inhibitor of NF-κB.Phase 1/2.

Chemical Structure

Molecular Weight: 456.7

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.88%

99.88

Related Targets	DNA/RNA Synthesis HDAC PPAR PARP Sirtuin ATM/ATR Casein Kinase eIF MDM2/MDMX DNA-PK DHFR Nucleoside Analog/Antimetabolite DNA alkylator Telomerase Thymidylate Synthase CRISPR/Cas9 RAD51 BMI-1 LIM kinase RNR Alkylating Agent NUDIX High-mobility Group OGG1 MTH1 G-quadruplex SMN FENs WRN Pax
Related Products	Camptothecin (CPT) (S)-10-Hydroxycamptothecin Beta-Lapachone Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Genz-644282 Hydroxy Camptothecine Rubitecan Eleutherin Clinafloxacin ABBV-969 Payload SW-044248 Cu(II)-Elesclomol Pefloxacin Mesylate Dihydrate Amsacrine hydrochloride Gepotidacin Topoisomerase IIα Antibody [H22C21] Cholesteryl hemisuccinate Dxd Ellipticine Exatecan 7-Ethylcamptothecin 9-amino-CPT (9-Aminocamptothecin) Amsacrine Topoisomerase I Antibody [C12J2] Belotecan (CKD-602) hydrochloride Topoisomerase IIα Antibody [E2A15] Flumequine Merbarone

Chemical Information, Storage & Stability

Molecular Weight	456.7	Formula	C₃₀H₄₈O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	472-15-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 20 mg/mL (43.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.
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.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.350mg/ml (5.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 47 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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 Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	HIV-1 ^[1] 1.4 μM(EC50) Eukaryotic topoisomerase I ^[3] 5 μM Aminopeptidase N ^[2] 7.3 μM
In vitro	Betulinic acid shows anti-HIV activity by blocking HIV replication in H9 lymphocytes with an EC50 value of 1.4 μM and inhibiting uninfected H9 cell growth with an IC50 value of 13 μM. ^[1] This compound also acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 μM. ^[2] In addition, it inhibits eukaryotic topoisomerase I activity with IC50 of 5 μM and can be exploited as a strong candidate for anti-tumor drug. ^[3]
Kinase Assay	Topoisomerase I-DNA interaction
Kinase Assay	Annealed 25-mer duplex of oligonucleotide-1 and oligonicleotide-2 is incubated with 25 or 50 units of rat liver topoisomerase I at 8 °C for 15 min in the presence or absence of betulinic acid in binding buffer. After incubation the reaction mixtures are electrophoresed in 7% non-denaturing polyacrylamide gel at 4 °C in 0.167 × TBE buffer and DNA bands are stained with ethidium bromid
In vivo	Betulinic acid inhibits prostate cancer cell and tumor (xenograft) growth in athymic nude mice bearing LNCaP cells and this is due, in part, to proteasome-dependent downregulation of Sp1, Sp3, Sp4 and several Sp-regulated genes. ^[4]
References	[1] https://pubmed.ncbi.nlm.nih.gov/8176401/ [2] https://pubmed.ncbi.nlm.nih.gov/9810272/ [3] https://pubmed.ncbi.nlm.nih.gov/12118187/ [4] https://pubmed.ncbi.nlm.nih.gov/17363604/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):