Cat. No.: HY-123467

Lasiokaurin

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Lasiokaurin is an anticancer agent. Lasiokaurin can be isolated from Rabdosia rubescens (Hemsl.) H. Hara. Lasiokaurin inhibits the function of the PDPK1-AKT axis, with a K_d value of 75.93 μM for PDPK1. Lasiokaurin inhibits mTOR, STAT3, MAPK and NF-κB. Lasiokaurin reduces the mRNA and protein expression levels of PLK1. Lasiokaurin decreases DNA synthesis levels, induces cell Apoptosis, and regulates Autophagy processes. Lasiokaurin inhibits tumor growth in xenograft models. Lasiokaurin can be used in research related to nasopharyngeal carcinoma, triple-negative breast cancer.

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Pureté: 99.68%
CAS No.: 28957-08-6
Formule: C₂₂H₃₀O₇
Masse moléculaire:406.47

Stockage:

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lasiokaurin Chemical Structure

CAS No.: 28957-08-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

PLK1

Voir tous les produits spécifiques à Isoform Polo-like Kinase (PLK) :

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	10.9 μM Compound: 8	Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK8 cells Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK8 cells	[PMID: 31200238]
A549	IC₅₀	13.47 μM Compound: 6	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
A549	IC₅₀	6.7 μM Compound: 19	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 23819871]
A549	IC₅₀	7.6 μM Compound: 13	Cytotoxicity against human A549 cells after 48 hrs by MTT method Cytotoxicity against human A549 cells after 48 hrs by MTT method	[PMID: 21534539]
B16	IC₅₀	32.57 μM Compound: 5	Antiproliferative activity against mouse B16 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against mouse B16 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31877536]
Bel-7402	IC₅₀	3.59 μM Compound: 6	Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
HCT-116	IC₅₀	13.48 μM Compound: 5	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31877536]
HepG2	IC₅₀	11.94 μM Compound: 5	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31877536]
HepG2	IC₅₀	5.67 μM Compound: 8	Antiproliferative activity against human HepG2 cells incubated for 72 hrs by CCK8 cells Antiproliferative activity against human HepG2 cells incubated for 72 hrs by CCK8 cells	[PMID: 31200238]
HL-60	IC₅₀	1.8 μM Compound: 19	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 23819871]
HL-60	IC₅₀	3.2 μM Compound: 13	Cytotoxicity against human HL60 cells after 48 hrs by MTT method Cytotoxicity against human HL60 cells after 48 hrs by MTT method	[PMID: 21534539]
K562	IC₅₀	4.92 μM Compound: 6	Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
K562	IC₅₀	521 μM Compound: 5	Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31877536]
L02	IC₅₀	22.36 μM Compound: 6	Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
L02	IC₅₀	25.39 μM Compound: 5	Cytotoxicity against human L02 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human L02 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 31877536]
MCF7	IC₅₀	19.82 μM Compound: 5	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31877536]
MCF7	IC₅₀	2.5 μM Compound: 19	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 23819871]
MCF7	IC₅₀	5.3 μM Compound: 13	Cytotoxicity against human MCF7 cells after 48 hrs by MTT method Cytotoxicity against human MCF7 cells after 48 hrs by MTT method	[PMID: 21534539]
PBMC	IC₅₀	>50 μM Compound: 5	Cytotoxicity against human PBMC cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human PBMC cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 31877536]
PBMC	IC₅₀	>50 μM Compound: 6	Cytotoxicity against human PBMC assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human PBMC assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
RAW264.7	IC₅₀	1.9 μM Compound: 19	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess method Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess method	[PMID: 23819871]
RPMI-8226	IC₅₀	11.03 μM Compound: 8	Antiproliferative activity against human RPMI8226 cells incubated for 72 hrs by CCK8 cells Antiproliferative activity against human RPMI8226 cells incubated for 72 hrs by CCK8 cells	[PMID: 31200238]
SGC-7901	IC₅₀	6.45 μM Compound: 6	Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
SMMC-7721	IC₅₀	2 μM Compound: 13	Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT method Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT method	[PMID: 21534539]
SMMC-7721	IC₅₀	2.7 μM Compound: 19	Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay	[PMID: 23819871]
SW480	IC₅₀	2.3 μM Compound: 13	Cytotoxicity against human SW480 cells after 48 hrs by MTT method Cytotoxicity against human SW480 cells after 48 hrs by MTT method	[PMID: 21534539]
SW480	IC₅₀	2.4 μM Compound: 19	Cytotoxicity against human SW480 cells after 48 hrs by MTT assay Cytotoxicity against human SW480 cells after 48 hrs by MTT assay	[PMID: 23819871]

In Vitro

Lasiokaurin (0.19-50 μM; 24-72 h) dose- and time-dependently inhibits the viability of CNE-1, CNE-2, and C666-1 nasopharyngeal carcinoma cells in vitro^[1].
Lasiokaurin (0.5-2 μM; 7 days) dose-dependently inhibits the colony formation of CNE-1 and CNE-2 nasopharyngeal carcinoma cells in vitro, with significant inhibition observed at concentrations as low as 0.5 μM^[1].
Lasiokaurin (2.5-10 μM; 24 h) dose-dependently inhibits the activation of MAPK, mTOR, STAT3, and NF-κB pathways in CNE-1 and CNE-2 nasopharyngeal carcinoma cells in vitro, including inhibition of both mTORC1 and mTORC2 complexes^[1].
Lasiokaurin (0.2-50 μM; 24-72 h) potently inhibits viability of MDA-MB-231, MDA-MB-468, and MCF7 breast cancer cells with IC₅₀ values ranging from 1.6 μM to 8.35 μM across 24-72 h, and exhibits lower toxicity to MCF-10A normal breast cells^[2].
Lasiokaurin (72 h) potently inhibits the viability of SK-BR-3, MDA-MB-231, BT-549, MCF-7, and T-47D human breast cancer cells with IC₅₀ values ranging from 1.59 μM to 4.16 μM after 72 h of treatment^[3].
Lasiokaurin (0.3-3 μM) inhibits the viability of patient-derived xenograft breast cancer organoids in a concentration-dependent manner^[3].
Lasiokaurin (2.5-10 μM; 24-48 h) induces dose- and time-dependent G2/M cell cycle arrest in CNE-1 and CNE-2 nasopharyngeal carcinoma cells in vitro by reducing cyclin B1 and cdc2 expression^[1].
Lasiokaurin (2.5-10 μM; 24 h) dose-dependently induces apoptosis in CNE-1 and CNE-2 nasopharyngeal carcinoma cells in vitro by increasing Bax expression^[1].
Lasiokaurin (2.5-5 μM; 12-48 h) dose- and time-dependently inhibits the migration of CNE-1 and CNE-2 nasopharyngeal carcinoma cells in vitro^[1].
Lasiokaurin (2.5-10 μM; 24-48 h) at concentrations of 2.5-10 μM induces DNA damage in MDA-MB-231 and MDA-MB-468 TNBC cells by suppressing PARP expression after 24 and 48 h of treatment^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

CNE-1, CNE-2, C666-1
Concentration:

0.19-50 μM
Incubation Time:

24 h; 48 h; 72 h
Result:

Caused a significant dose- and time-dependent reduction in cell viability across all three NPC cell lines.
Inhibited cell viability with statistically significant effects (p < 0.05, p < 0.001) observed at multiple concentration-time combinations.

Cell Cycle Analysis^[1]

Cell Line:

CNE-1, CNE-2
Concentration:

2.5-10 μM
Incubation Time:

24 h; 48 h
Result:

Caused a dose- and time-dependent increase in the proportion of cells in the G2/M phase.
Reduced cyclin B1 and cdc2 protein expression in both cell lines at 2.5, 5, and 10 μM (24 h incubation), with statistically significant decreases observed at 5 μM and 10 μM (p < 0.05, p < 0.01).

Apoptosis Analysis^[1]

Cell Line:

CNE-1, CNE-2
Concentration:

2.5-10 μM
Incubation Time:

24 h
Result:

Caused a dose-dependent increase in the percentage of apoptotic cells (early and late apoptosis) in both cell lines.
Increased Bax expression in CNE-1 cells at 2.5 μM, 5 μM, and 10 μM, with significant elevations at 5 μM and 10 μM (p < 0.01).
Increased Bax expression in CNE-2 cells at 2.5 μM, 5 μM, and 10 μM, with significant elevations at 5 μM (p < 0.05) and 10 μM (p < 0.01).

Cell Migration Assay ^[1]

Cell Line:

CNE-1, CNE-2
Concentration:

2.5-5 μM
Incubation Time:

12 h; 24 h; 36 h; 48 h
Result:

Caused a dose- and time-dependent reduction in relative wound healing rates in both cell lines.
Resulted in significantly lower wound healing rates compared to controls at all time points with 5 μM Lasiokaurin, with 2.5 μM Lasiokaurin also showing inhibitory effects.

Western Blot Analysis^[1]

Cell Line:

CNE-1, CNE-2
Concentration:

2.5-10 μM
Incubation Time:

24 h
Result:

Dose-dependently reduced phosphorylation of Erk1/2, p38, mTOR, STAT3, and NF-κB in both cell lines, with significant decreases observed at multiple concentrations (p < 0.05, p < 0.01).
Reduced expression of Rictor, Raptor, and Gβl (components of mTORC1 and mTORC2) in both cell lines, with significant decreases at 5 μM and 10 μM (p < 0.05, p < 0.01).

In Vivo

Lasiokaurin (10-20 mg/kg; i.p.; daily; 12 days) inhibits nasopharyngeal carcinoma xenograft tumor growth in BALB/c nude mice, with the 20 mg/kg dose producing a greater reduction in tumor volume and weight, while maintaining stable mouse body weights^[1].
Lasiokaurin (5-10 mg/kg; i.p.; daily; 20 days) significantly inhibits triple-negative breast cancer xenograft tumor growth in BALB/c nude mice, with the 10 mg/kg dose showing efficacy comparable to docetaxel and no detectable toxicity to vital organs or body weight^[2].
Lasiokaurin (7.5-15 mg/kg; i.p.; once every 2 days; 27 days) inhibits breast cancer growth in vivo by suppressing PLK1 pathway signaling, with 15 mg/kg lasiokaurin significantly reducing tumor volume, tumor weight, and cell proliferation while inducing apoptosis, without causing significant body weight loss^[3].
Lasiokaurin (25 mg/kg; i.p.; once every two days) significantly inhibits breast cancer xenograft growth in nude mice by activating autophagy, inhibiting the AKT/mTOR signaling pathway, and suppressing glycolytic activity, with no observed toxicity^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude mice (female, housed at 23°C with 12 h light/dark cycle)^[2]
Dosage:

5 mg/kg; 10 mg/kg
Administration:

i.p.; daily; 20 days
Result:

Significantly reduced tumor volume and tumor weight relative to the vehicle group.
Showed slightly lower efficacy than docetaxel at 5 mg/kg.
Demonstrated comparable efficacy to docetaxel at 10 mg/kg.
Caused no significant effect on mouse body weight.
Showed no notable alterations in organ weight or histopathological characteristics of heart, lung, liver, spleen, or kidney relative to the vehicle group.

Animal Model:

Balb/c nude (female, 5 weeks old, 18-22 g, subcutaneous xenograft model)^[3]
Dosage:

7.5 mg/kg; 15 mg/kg
Administration:

i.p.; once every 2 days; 27 days
Result:

Significantly reduced tumor volume and tumor weight at 15 mg/kg compared to vehicle controls.
Showed no significant body weight loss relative to vehicle controls.
Significantly reduced Ki67 expression in tumor tissue.
Significantly increased TUNEL-positive cells in tumor tissue.
Downregulated tumor tissue protein levels of PLK1, CDC25C, CyclinB1, CDC2, and p-AKT relative to total AKT.

Animal Model:

Nude mice (female, six-week-old)^[4]
Dosage:

25 mg/kg
Administration:

i.p.; once every two days; 9 total doses
Result:

Significantly reduced xenograft tumor growth compared to PBS control, with lower final tumor weights and slower tumor volume progression over 18 days.
Reduced Ki67-positive proliferating cells in tumor tissues.
Increased TUNEL-positive apoptotic cells and necrotic area in tumor tissues.
Increased LC3II levels in tumor tissues.
Decreased PDPK1 expression in tumor tissues.
Increased protein levels of p62, beclin1, ATG5, and LC3II in tumor tissues.
Decreased phosphorylated levels of AKT, mTOR, and p70S6K in tumor tissues.
Reduced protein levels of glycolysis-related markers HK2, GLUT1, GLUT3, and LDHA in tumor tissues.
Maintained stable mouse body weights with no treatment-related damage observed in heart, liver, spleen, lung, and kidney via H&E staining.

Chemical Information

CAS No. 28957-08-6
Appearance Solid
Masse moléculaire 406.47
Formule C₂₂H₃₀O₇
Color White to off-white
SMILES

O[C@]1(OC2)[C@]([C@@H]3O)(C4=O)[C@](CC[C@H]3C4=C)([H])[C@]2([C@H](CC5)OC(C)=O)[C@](C5(C)C)([H])[C@@H]1O
Structure Classification
- Terpenoids
- Diterpenoids
Initial Source
- Plants
- Labiatae
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (1)

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Biochem Pharmacol

Lasiokaurin suppresses breast cancer growth by blocking autophagic flux and regulating cellular energy homeostasis. [Abstract]

2025 Aug 7;242(Pt 3):117212. PMID: 40782951

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (246.02 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

2.4602 mL

12.3010 mL

24.6021 mL

5 mM

0.4920 mL

2.4602 mL

4.9204 mL

10 mM

0.2460 mL

1.2301 mL

2.4602 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
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g
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μL
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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:

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (301 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
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Références

[1]. Pu H, et al. Exploring the in vitro and in vivo anticancer activity of lasiokaurin on nasopharyngeal carcinoma[J]. Pharmacological Research-Modern Chinese Medicine, 2023, 9: 100303.

[2]. Lin J, et al. In Vitro and In Vivo Anti-Cancer Activity of Lasiokaurin in a Triple-Negative Breast Cancer Model. Molecules (Basel, Switzerland). 2023 Nov 22;28(23):7701.

[3]. Liu Z, et al. Lasiokaurin Regulates PLK1 to Induce Breast Cancer Cell G2/M Phase Block and Apoptosis. Journal of Cancer. 2024;15(8):2318-2328. [Content Brief]

[4]. Huang R, et al. Lasiokaurin suppresses breast cancer growth by blocking autophagic flux and regulating cellular energy homeostasis. Biochemical pharmacology. 2025 Dec;242(Pt 3):117212. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4602 mL	12.3010 mL	24.6021 mL	61.5052 mL
	5 mM	0.4920 mL	2.4602 mL	4.9204 mL	12.3010 mL
	10 mM	0.2460 mL	1.2301 mL	2.4602 mL	6.1505 mL
	15 mM	0.1640 mL	0.8201 mL	1.6401 mL	4.1003 mL
	20 mM	0.1230 mL	0.6151 mL	1.2301 mL	3.0753 mL
	25 mM	0.0984 mL	0.4920 mL	0.9841 mL	2.4602 mL
	30 mM	0.0820 mL	0.4100 mL	0.8201 mL	2.0502 mL
	40 mM	0.0615 mL	0.3075 mL	0.6151 mL	1.5376 mL
	50 mM	0.0492 mL	0.2460 mL	0.4920 mL	1.2301 mL
	60 mM	0.0410 mL	0.2050 mL	0.4100 mL	1.0251 mL
	80 mM	0.0308 mL	0.1538 mL	0.3075 mL	0.7688 mL
	100 mM	0.0246 mL	0.1230 mL	0.2460 mL	0.6151 mL

Lasiokaurin

1 Cited Publications

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Lasiokaurin

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Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Lasiokaurin Related Classifications

Cat. No.: HY-123467