Art. -Nr.: HY-149324

SP27

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SP27 is a PROTAC PLK4 degrader with an IC₅₀ of 8.4 nM and a DC₅₀ of 19.5 nM against PLK4. SP27 induces PLK4 degradation via the CRBN-dependent ubiquitin-proteasome pathway, inhibits PLK4 downstream signal transduction, and suppresses the growth of TRIM37-amplified breast cancer cells. SP27 is applicable for breast cancer-related research.
(Pink: PLK4 ligand (HY-128493); Blue: Cereblon ligand (HY-14658); Black: linker).

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Reinheit: 98.87%
CAS. Nr.: 3034805-75-6
Formel: C₄₀H₄₀F₂N₁₂O₅
Molecular Weight:806.82

Speicherung:

4°C, protect from light

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

SP27 Chemical Structure

CAS. Nr.: 3034805-75-6

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Preis

Verfügbarkeit

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SP27 is a PROTAC PLK4 degrader with an IC₅₀ of 8.4 nM and a DC₅₀ of 19.5 nM against PLK4. SP27 induces PLK4 degradation via the CRBN-dependent ubiquitin-proteasome pathway, inhibits PLK4 downstream signal transduction, and suppresses the growth of TRIM37-amplified breast cancer cells. SP27 is applicable for breast cancer-related research^[1]. (Pink: PLK4 ligand (HY-128493); Blue: Cereblon ligand (HY-14658); Black: linker).

IC₅₀ & Target^[1]

PLK4

8.4 nM (IC₅₀)

PLK4

19.5 nM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	0.073 μM Compound: SP27	Antiproliferative activity against human MCF7 cells incubated for 5 days by CCK-8 assay Antiproliferative activity against human MCF7 cells incubated for 5 days by CCK-8 assay	[PMID: 37279162]

In Vitro

SP27 potently binds to purified PLK4 protein with an IC₅₀ of 8.4 nM; it potently inhibits the proliferation of TRIM37-amplified MCF-7 breast cancer cells with an IC₅₀ of 0.073 μM^[1].
SP27 exhibits favorable in vitro metabolic stability in human plasma as well as liver microsomes from humans, rats and mice, and shows extremely weak inhibitory effects on major CYP450 isoforms, suggesting a low risk of drug-drug interactions^[1].
SP27 (0.1-10 μM; 48 h) induces concentration-dependent degradation of PLK4 in TRIM37-amplified MCF-7 breast cancer cells, with a DC₅₀ of 19.5 nM; it induces PLK4 degradation in TRIM37-amplified MCF-7 breast cancer cells via the CRBN-dependent ubiquitin-proteasome pathway^[1].
SP27 inhibits the downstream signaling pathway of PLK4 in TRIM37-amplified MCF-7 breast cancer cells in a concentration-dependent manner by reducing FBXW5 inactivation and promoting SAS-6 degradation^[1].
SP27 (1 μM; 48 h) exhibits favorable proteome selectivity for PLK4 in TRIM37-amplified MCF-7 breast cancer cells, and its anti-tumor activity is associated with the p53 signaling pathway^[1].
SP27 (0.05-2.00 μM) inhibits colony formation, induces apoptosis and G₂ phase cell cycle arrest, promotes cellular senescence (48 h), and suppresses the migration of TRIM37-amplified MCF-7 breast cancer cells in a concentration-dependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:

TRIM37-amplified MCF-7 breast cancer cells
Concentration:

0.1, 1, 10 μM
1 nM, 3 nM, 10 nM, 300 nM, 1 μM, 3 μM, 10 μM (DC₅₀ test)
Incubation Time:

48 h
Result:

Induced PLK4 degradation in a concentration-dependent manner, with 68.3% degradation at 0.1 μM, 73.4% degradation at 1 μM, and 83.5% degradation at 10 μM after 48 h of treatment.
Achieved a half-maximal degradation concentration (DC₅₀) of 19.5 nM, with no observed hook effect at 10 μM.

Cell Migration Assay ^[1]

Cell Line:

MCF-7 breast cancer cells
Concentration:

0.1, 0.3, 1 μM
Incubation Time:

24, 48 h
Result:

Inhibited the migration of MCF-7 cells in a wound healing assay.

Parmacokinetics

Species	Dose	Route	AUC_last	AUC_{INF_obs}	T_1/2	CL	V_{ss_obs}	MRT_0-∞	T_max	C_max	Bioavailability
Mice^[1]	2 mg/kg	i.v.	941 ng·h/mL	956 ng·h/mL	5.34 h	34.9 mL/min/kg	16277 mL/kg	2.29 h	/	/	/
Mice^[1]	20 mg/kg	i.p.	14038 ng·h/mL	14230 ng·h/mL	4.66 h	/	/	3.93 h	1.42 h	4567 ng/mL	149 %

In Vivo

SP27 (20 mg/kg; i.p.; once every other day; 21 days) exhibits potent in vivo antitumor efficacy in TRIM37-amplified breast cancer xenografts, with a 73.7% tumor growth inhibition rate, while maintaining good tolerability in mice^[1].

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

Chemical Information

CAS. Nr. 3034805-75-6
Appearance Solid
Molecular Weight 806.82
Formel C₄₀H₄₀F₂N₁₂O₅
Color Light yellow to yellow
SMILES

FC1=CC=C(C(F)=C1)CNC2=NC3=C(C=NN3C4CCN(CC4)C(C5CCN(CC5)C6=CC7=C(C=C6)C(N(C7=O)C8C(NC(CC8)=O)=O)=O)=O)C(NC9=NNC(C)=C9)=N2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (123.94 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

1.2394 mL

6.1972 mL

12.3943 mL

5 mM

0.2479 mL

1.2394 mL

2.4789 mL

10 mM

0.1239 mL

0.6197 mL

1.2394 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.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 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]. Sun Y, et al. Discovery of the First Potent, Selective, and Efficacious Polo-like Kinase 4 Proteolysis Targeting Chimera Degrader for the Treatment of -Amplified Breast Cancer. Journal of medicinal chemistry. 2023 Jun 22;66(12):8200-8221. [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	1.2394 mL	6.1972 mL	12.3943 mL	30.9858 mL
	5 mM	0.2479 mL	1.2394 mL	2.4789 mL	6.1972 mL
	10 mM	0.1239 mL	0.6197 mL	1.2394 mL	3.0986 mL
	15 mM	0.0826 mL	0.4131 mL	0.8263 mL	2.0657 mL
	20 mM	0.0620 mL	0.3099 mL	0.6197 mL	1.5493 mL
	25 mM	0.0496 mL	0.2479 mL	0.4958 mL	1.2394 mL
	30 mM	0.0413 mL	0.2066 mL	0.4131 mL	1.0329 mL
	40 mM	0.0310 mL	0.1549 mL	0.3099 mL	0.7746 mL
	50 mM	0.0248 mL	0.1239 mL	0.2479 mL	0.6197 mL
	60 mM	0.0207 mL	0.1033 mL	0.2066 mL	0.5164 mL
	80 mM	0.0155 mL	0.0775 mL	0.1549 mL	0.3873 mL
	100 mM	0.0124 mL	0.0620 mL	0.1239 mL	0.3099 mL

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SP27

PROTAC Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SP27

PROTAC Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SP27 Related Classifications

HY-149324 Related Classifications