Art. -Nr.: HY-178164

HBS-101

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HBS-101 is a selectively, orally active, brain-penetrant, Midkine (MDK) inhibitor (K_D = 38.4 nM). HBS-101 significantly reduces cell viability, clonogenic survival, and invasiveness and increases apoptosis. HBS-101 involves suppression of the Akt/mTOR, STAT3, and NF-κB pathways. HBS-101 can be used for the study of Triple-negative breast cancer (TNBC).

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Reinheit: 99.59%
Formel: C₂₁H₂₄F₂O₂
Molecular Weight:346.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

HBS-101 Chemical Structure

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

In Vitro

HBS-101 (0.1-10 μM, 5 days) significantly reduces cell viability of TNBC cell lines^[1].
HBS-101 (0-5 μM) reduces the colony-forming ability of TNBC cells in a dose-dependent manner^[1].
HBS-101 (20 μM, 24 h) induces apoptosis in TNBC cells, but not in normal mammary epithelial cells^[1].
HBS-101 (20 μM, 20 h) significantly reduces the expression of MDK receptors, specifically Notch2, in HCC-70 cells; inhibits downstream signaling pathways, including mTOR, STAT3, and NF-κB; and increases cleaved caspase-3 levels^[1].
HBS-101 (20 μM, 24 h) downregulates MDK target genes and significantly reduces STAT3 and NF-κB reporter activity in TNBC cells that stably express these reporters^[1].

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

Cell Viability Assay^[1]

Cell Line:

SUM-159, BT-549, MDA-MB-468, MDA-MB-231, MDA-MB-231-BrM2-831, HCC-70, HCC-1937, HER2+ SKBR3, ER+ MCF7, MCF10A
Concentration:

0.1 μM, 1 μM, 10 μM
Incubation Time:

5 days
Result:

Significantly inhibited the viability of TNBC cell lines, with IC₅₀ values ranging from 0.3 to 2.8 μmol/L.
Exhibited weaker inhibitory effects on HER2+ SKBR3, (IC₅₀ ~ 16 μM) and ER+MCF7, (IC₅₀ > 20 μM) breast cancer cell lines.
Showed no toxicity against normal breast epithelial MCF10A cells.

Western Blot Analysis^[1]

Cell Line:

HCC-70 cells
Concentration:

20 μM
Incubation Time:

20 h
Result:

Reduced Notch2 receptor protein levels.
Inhibited the phosphorylation of mTOR, STAT3, and NF-κB, and increased the level of cleaved caspase-3, a marker of apoptosis.

RT-PCR^[1]

Cell Line:

MDA-MB-231 cells, BT-549 cells
Concentration:

20 μM
Incubation Time:

20 h
Result:

Significantly reduced STAT3 and NF-κB reporter activity in TNBC cells that stably express these reporters.

Cell Invasion Assay^[1]

Cell Line:

MDA-MB-231 cells, BT-549 cells, MCF10A cells
Concentration:

20 μM
Incubation Time:

24 h
Result:

Induced apoptosis in TNBC cells, but not in normal mammary epithelial cells.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_inf	T_1/2	CL/F
Rat	10 mg/kg	i.p.	0.54 h	6271 ng/mL	5233 ng·h/mL	0.52 h	1971 mL/h/kg

In Vivo

HBS-101 (1 mg/kg (i.v.), 10 mg/kg (p.o.) has rapid in vivo disposition kinetics and extremely high oral bioavailability in rats^[1].
HBS-101 (10 mg/kg, i.p.) can be rapidly absorbed and effectively penetrates the blood-brain barrier in mice^[1].
HBS-101 (2-10 mg/kg, p.o., 5 days) doses up to 10 mg/kg (oral) for 5 consecutive days are safe and do not produce observable organ toxicity in mice^[1].
HBS-101 (2 mg/kg, 5 mg/kg, p.o., 5 days) effectively inhibits the growth of TNBC orthotopic tumors with oral administration, and 5 mg/kg is determined to be the minimum effective dose in mice^[1].
HBS-101 (5 mg/kg, p.o., 5 days a week) reduces the proliferative activity of tumors in MDA-MB-231 cells xenograft mice^[1].
HBS-101 (10 mg/kg, i.p., 5 days a week) exhibits potent anti-tumor activity in a brain metastasis model in mice^[1].

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

Animal Model:

Rats^[1].
Dosage:

1 mg/kg, 10 mg/kg
Administration:

I.v., p.o.
Result:

Had monoexponential disposition in vivo and had an estimated plasma half-life between 0.7 and 1.6 hours.
Had excellent oral bioavailability in rats.

Animal Model:

Female C57BL/6 mice^[1].
Dosage:

10 mg/kg
Administration:

I.p., once
Result:

Absorbed rapidly following i.p. administration, resembling an i.v. bolus drug administration.
Detected in the brain, with peak detectable levels reaching 1,654 ng/g 10 minutes after administration, suggesting that HBS-101 effectively crosses the blood-brain barrier.

Animal Model:

Female C57BL/6 mice^[1].
Dosage:

2 mg/kg, 5 mg/kg, 10 mg/kg
Administration:

P.o., 5 days
Result:

No abnormalities were detected during the gross pathological examination of the animals.

Animal Model:

MDA-MB-231 cells (2 × 10⁶) mixed with a 1:1 volume of Matrigel were injected into the mammary fat pad of the nude mice^[1].
Dosage:

2 mg/kg, 5 mg/kg
Administration:

P.o., 5 times a week
Result:

Led to a significant dose-dependent reduction in tumor volume.
Not affected mouse body weight.
Significant decreased in Ki-67–positive cells.

Animal Model:

Female SCID mice were used as recipients for 2 mm³ TNBC–PDX-96 tumor tissue implants to establish subcutaneous PDX tumor models^[1].
Dosage:

5 mg/kg
Administration:

P.o., 5 times a week
Result:

Significantly inhibited PDX tumor growth, with tumor volume and weight significantly reduced. Significant decrease in Ki-67-positive cells.

Animal Model:

1.75 × 10⁵ brain-metastatic MDA-MB-231-BrM2-831 cells were orthotopically injected into the right cerebral hemisphere of female NOD.CB17-Prkdcscid/NCrCrl mice^[1].
Dosage:

10 mg/kg
Administration:

I.p., 5 times a week
Result:

Significantly reduced tumor progression and extended the survival of mice with orthotopic tumors.

Chemical Information

Appearance Solid
Molecular Weight 346.41
Formel C₂₁H₂₄F₂O₂
Color White to off-white
SMILES

C[C@@]12[C@](O)(C(F)(F)C#C)CC[C@@]1([H])[C@]3([H])CCC4=CC(CCC4=C3CC2)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (288.68 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

2.8868 mL

14.4338 mL

28.8675 mL

5 mM

0.5774 mL

2.8868 mL

5.7735 mL

10 mM

0.2887 mL

1.4434 mL

2.8868 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mahajan M, et al. The Discovery and Characterization of HBS-101, a Novel Inhibitor of Midkine, as a Therapeutic Agent for the Treatment of Triple-Negative Breast Cancer. Mol Cancer Ther. 2025 Sep 2;24(9):1308-1319. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8868 mL	14.4338 mL	28.8675 mL	72.1688 mL
	5 mM	0.5774 mL	2.8868 mL	5.7735 mL	14.4338 mL
	10 mM	0.2887 mL	1.4434 mL	2.8868 mL	7.2169 mL
	15 mM	0.1925 mL	0.9623 mL	1.9245 mL	4.8113 mL
	20 mM	0.1443 mL	0.7217 mL	1.4434 mL	3.6084 mL
	25 mM	0.1155 mL	0.5774 mL	1.1547 mL	2.8868 mL
	30 mM	0.0962 mL	0.4811 mL	0.9623 mL	2.4056 mL
	40 mM	0.0722 mL	0.3608 mL	0.7217 mL	1.8042 mL
	50 mM	0.0577 mL	0.2887 mL	0.5774 mL	1.4434 mL
	60 mM	0.0481 mL	0.2406 mL	0.4811 mL	1.2028 mL
	80 mM	0.0361 mL	0.1804 mL	0.3608 mL	0.9021 mL
	100 mM	0.0289 mL	0.1443 mL	0.2887 mL	0.7217 mL

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HBS-101

Apoptosis Compound Library

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High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alkyne Compound Library

Alle Akt Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HBS-101 Related Classifications

HY-178164 Related Classifications