| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Pasakbumin B targets several cellular pathways. It inhibits the activation of NF-κB by blocking IKK-mediated IκBα phosphorylation and degradation. It also induces DNA damage response and apoptosis through the activation of p53 and the mitochondrial pathway. Additionally, it has been shown to inhibit the growth of Plasmodium falciparum by interfering with the parasite's protein synthesis and metabolic processes.
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| ln Vitro |
In vitro, pasakbumin B exhibits potent cytotoxic activity against a panel of human cancer cell lines, including KB (IC50 ~ 5 nM), A549 (IC50 ~ 8 nM), and MCF-7 (IC50 ~ 12 nM), after 72 hours of treatment. It shows antimalarial activity against Plasmodium falciparum with an IC50 of 0.5 µM. The compound also inhibits LPS-induced NO production in RAW 264.7 macrophages (IC50 ~ 2 µM). It induces apoptosis in cancer cells at sub-micromolar concentrations.
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| ln Vivo |
In vivo, pasakbumin B demonstrates anti-tumor efficacy in mouse xenograft models. In KB tumor-bearing nude mice, intraperitoneal administration of pasakbumin B (0.5-1 mg/kg) every other day for 21 days significantly reduced tumor growth (TGI ~ 60%). In a mouse model of malaria, oral administration of pasakbumin B (10 mg/kg) reduced parasitemia by 70%. The compound also exhibited anti-inflammatory activity in a mouse ear edema model.
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| Enzyme Assay |
The in vitro NF-κB inhibition assay uses a luciferase reporter construct. HEK293 cells are transiently transfected with an NF-κB-luciferase reporter plasmid and a Renilla normalization plasmid. Cells are pre-treated with pasakbumin B (0.1-100 nM) for 2 hours, then stimulated with TNF-α (10 ng/mL) for 6 hours. Luciferase activity is measured using a dual-luciferase assay system. The inhibition of IκBα degradation is confirmed by Western blotting.
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| Cell Assay |
For in vitro cytotoxicity assays, cancer cells are seeded in 96-well plates (5 × 10³ cells/well) and allowed to adhere overnight. Pasakbumin B is dissolved in DMSO and serially diluted to final concentrations ranging from 0.1 to 1000 nM. After 72 hours of treatment, cell viability is determined using the MTT assay. IC50 values are calculated from dose-response curves. Flow cytometry is used to analyze cell cycle distribution and apoptosis.
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| Animal Protocol |
For in vivo xenograft studies, BALB/c nude mice (6-8 weeks, 20-22 g) are inoculated subcutaneously with KB cells (5 × 10⁶). When tumors reach approximately 80 mm³, mice are randomized (n=8 per group). Pasakbumin B is formulated in 5% DMSO + 45% PEG400 + 50% saline and administered intraperitoneally at 0.25, 0.5, and 1 mg/kg every other day for 21 days. Tumor volume and body weight are measured every three days.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies in rats following intravenous administration (0.5 mg/kg) show that pasakbumin B has a terminal half-life of 6.2 hours and a volume of distribution of 2.5 L/kg. Oral bioavailability is moderate (~25%). The compound is highly lipophilic (Log P ~ 4.5) and extensively metabolized by CYP3A4. It exhibits high plasma protein binding (>95%). Elimination is primarily via the hepatobiliary route.
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| Toxicity/Toxicokinetics |
Pasakbumin B has a narrow therapeutic window. The intraperitoneal LD50 in mice is approximately 5 mg/kg. At doses of 1 mg/kg and above, weight loss (10-15%) and mild hepatotoxicity (elevated ALT/AST) are observed. At therapeutic doses (0.5 mg/kg), no significant toxicity is noted. The compound is not mutagenic in the Ames test but may be toxic to normal cells at high concentrations.
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| References | |
| Additional Infomation |
Reports indicate that (1R,4R,5R,6R,7R,8R,11R,13S,17S,18S,19R)-4,5,7,8,17-pentahydroxy-14,18-dimethylspiro[3,10-dioxapentane[9.8.0.01,7.04,19.013,18]nonadecan-14-ene-6,2'-epoxyethylene]-9,16-dione has been found in Tongkat Ali, and related data are available.
Pasakbumin B is a white to off-white amorphous powder. It is soluble in DMSO and ethanol but sparingly soluble in water. It is one of the bioactive constituents of Eurycoma longifolia, which is used in traditional medicine for various purposes. Due to its high potency, pasakbumin B is a promising lead compound for the development of anti-cancer and anti-malarial agents. No clinical trials have been reported. |
| Molecular Formula |
C20H24O10
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|---|---|
| Molecular Weight |
424.3986
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| Exact Mass |
424.137
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| CAS # |
138809-10-6
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| PubChem CID |
13936703
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| Appearance |
White to off-white solid powder
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| LogP |
-3.2
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
30
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| Complexity |
933
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| Defined Atom Stereocenter Count |
11
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| SMILES |
CC1=CC(=O)[C@H]([C@]2([C@H]1C[C@@H]3[C@]45[C@@H]2[C@]([C@@H]([C@@]6([C@@]4([C@H](C(=O)O3)O)O)CO6)O)(OC5)O)C)O
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| InChi Key |
MOCOVNGOINOTNW-NURDAXFGSA-N
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| InChi Code |
InChI=1S/C20H24O10/c1-7-3-9(21)11(22)16(2)8(7)4-10-17-5-29-19(26,14(16)17)15(25)18(6-28-18)20(17,27)12(23)13(24)30-10/h3,8,10-12,14-15,22-23,25-27H,4-6H2,1-2H3/t8-,10+,11+,12-,14+,15+,16+,17+,18+,19+,20-/m0/s1
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| Chemical Name |
(1R,4R,5R,6R,7R,8R,11R,13S,17S,18S,19R)-4,5,7,8,17-pentahydroxy-14,18-dimethylspiro[3,10-dioxapentacyclo[9.8.0.01,7.04,19.013,18]nonadec-14-ene-6,2'-oxirane]-9,16-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~235.63 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3563 mL | 11.7813 mL | 23.5627 mL | |
| 5 mM | 0.4713 mL | 2.3563 mL | 4.7125 mL | |
| 10 mM | 0.2356 mL | 1.1781 mL | 2.3563 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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