Art. -Nr.: HY-128756

SIAIS178

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SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC₅₀ of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.
(Pink: Bcr-Abl ligand (HY-107447); Blue: VHL ligand (HY-125845); Black: linker (HY-W015300)).

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Reinheit: 98.64%
CAS. Nr.: 2376047-73-1
Formel: C₅₀H₆₂ClN₁₁O₆S₂
Molecular Weight:1012.68

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SIAIS178 Chemical Structure

CAS. Nr.: 2376047-73-1

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Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC₅₀ of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity^[1]. (Pink: Bcr-Abl ligand (HY-107447); Blue: VHL ligand (HY-125845); Black: linker (HY-W015300)).

IC₅₀ & Target^[1]

VHL	Bcr-Abl 24 nM (IC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen :

Abl
Bcr-Abl

Cellular Effect

Cell Line	Type	Value	Description	References
K562	DC₅₀	8.5 nM Compound: 19; SIAIS178	Protac activity against VHL/BCR-ABL in human K562 cells assessed as induction of BCR-ABL degradation by Western blot analysis Protac activity against VHL/BCR-ABL in human K562 cells assessed as induction of BCR-ABL degradation by Western blot analysis	[PMID: 31539241]
K562	IC₅₀	24 nM Compound: 19; SIAIS178	Growth inhibition of human K562 cells incubated for 2 days by CCK8 assay Growth inhibition of human K562 cells incubated for 2 days by CCK8 assay	[PMID: 31539241]

In Vitro

SIAIS178 (1-100 nM; for 16 hours) significantly reduces the BCR-ABL protein levels in a concentration dependent manner. SIAIS178 significantly inhibits the phosphorylation of BCR-ABL and the substrates STAT5^[1].
SIAIS178 (1, 10, 100, 1000 nM) exerts significant antiproliferative activity in BCR-ABL driven CML cell lines. SIAIS178 retains potency and selectivity against the BCR-ABL driven cell lines^[1].

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

Western Blot Analysis^[1]

Cell Line:

K562 cells
Concentration:

1, 3, 10, 30, 100 nM
Incubation Time:

16 hours
Result:

Significantly reduced the BCR-ABL protein levels in a concentration dependent manner.

In Vivo

SIAIS178 (ip; 5, 15, and 45 mg/kg; 12 days) attenuates tumor progression in a dose-dependent manner, as determined by serial volumetric measurement ^[1].
SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T_1/2 of 3.82 and 12.35 hours and C_max of 1165.2 nM and 30 nM for iv and ip, respectively^[1].

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

Animal Model:

NOD/SCID mice with termed K562-Luc^[1]
Dosage:

5, 15, and 45 mg/kg
Administration:

Ip; 12 days
Result:

Attenuated tumor progression in a dose-dependent manner, as determined by serial volumetric measurement.

Animal Model:

Female Wistar rats^[1]
Dosage:

2 mg/kg (Pharmacokinetic Analysis)
Administration:

Iv or ip; 24 hours
Result:

Had T_1/2 of 3.82 and 12.35 hours and C_max of 1165.2 nM and 30 nM for iv and ip, respectively.

Chemical Information

CAS. Nr. 2376047-73-1
Appearance Solid
Molecular Weight 1012.68
Formel C₅₀H₆₂ClN₁₁O₆S₂
Color White to off-white
SMILES

O=C(N1CCN(C2=NC(C)=NC(NC3=NC=C(C(NC4=C(C=CC=C4Cl)C)=O)S3)=C2)CC1)CCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@@H](O)C5)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 300 mg/mL (296.24 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

0.9875 mL

4.9374 mL

9.8748 mL

5 mM

0.1975 mL

0.9875 mL

1.9750 mL

10 mM

0.0987 mL

0.4937 mL

0.9875 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 7.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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.

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 (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Zhao Q, et al. Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. J Med Chem. 2019 Oct 24;62(20):9281-9298. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	0.9875 mL	4.9374 mL	9.8748 mL	24.6870 mL
	5 mM	0.1975 mL	0.9875 mL	1.9750 mL	4.9374 mL
	10 mM	0.0987 mL	0.4937 mL	0.9875 mL	2.4687 mL
	15 mM	0.0658 mL	0.3292 mL	0.6583 mL	1.6458 mL
	20 mM	0.0494 mL	0.2469 mL	0.4937 mL	1.2343 mL
	25 mM	0.0395 mL	0.1975 mL	0.3950 mL	0.9875 mL
	30 mM	0.0329 mL	0.1646 mL	0.3292 mL	0.8229 mL
	40 mM	0.0247 mL	0.1234 mL	0.2469 mL	0.6172 mL
	50 mM	0.0197 mL	0.0987 mL	0.1975 mL	0.4937 mL
	60 mM	0.0165 mL	0.0823 mL	0.1646 mL	0.4114 mL
	80 mM	0.0123 mL	0.0617 mL	0.1234 mL	0.3086 mL
	100 mM	0.0099 mL	0.0494 mL	0.0987 mL	0.2469 mL

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SIAIS178

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Cytoskeleton Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Blood Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SIAIS178

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Cytoskeleton Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Blood Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SIAIS178 Related Classifications

HY-128756 Related Classifications