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SIAIS178

Name: SIAIS178
Brand: TargetMol
SKU: T12907
Price: 163 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12907Cas No. 2376047-73-1

Alias SIAI S178

SIAIS178 is a selective PROTAC degrader targeting BCR-ABL with an IC50 of 24 nM. It degrades BCR-ABL protein by recruiting the VHL E3 ubiquitin ligase, inhibiting leukaemia cell growth in vitro and causing regression of K562 xenograft tumours.

SIAIS178

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Purity: 98.07%

Catalog No. T12907Alias SIAI S178Cas No. 2376047-73-1

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$163	-	In Stock
5 mg	$396	-	In Stock
10 mg	$538	-	In Stock
25 mg	$987	-	In Stock
50 mg	$1,590	-	In Stock
100 mg	$2,280	-	In Stock
200 mg	$2,970	-	In Stock
1 mL x 10 mM (in DMSO)	$436	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.07%

Appearance:Solid

Color:Yellow

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COA

Product Introduction

Bioactivity

Description	SIAIS178 is a selective PROTAC degrader targeting BCR-ABL with an IC50 of 24 nM. It degrades BCR-ABL protein by recruiting the VHL E3 ubiquitin ligase, inhibiting leukaemia cell growth in vitro and causing regression of K562 xenograft tumours.
Targets&IC50	VHL:24 nM, BCR-ABL:24 nM
In vitro	Methods: K562 cells were treated with SIAIS178 (1, 3, 10, 30, 100 nM, 16 hours) and BCR-ABL protein expression was detected by Western blot. Results: SIAIS178 significantly reduced BCR-ABL protein levels in a concentration-dependent manner. [1]
In vivo	Methods: SIAIS178 (5, 15, and 45 mg/kg) was used to treat K562-Luc NOD/SCID mice and investigate its effect on tumor progression in vivo. Results: SIAIS178 attenuated tumor progression in a dose-dependent manner as determined by serial volume measurements. [1]
Synonyms	SIAI S178

Chemical Properties

Molecular Weight	1012.68
Formula	C₅₀H₆₂ClN₁₁O₆S₂
Cas No.	2376047-73-1
Smiles	C([C@@H](NC(CCCCCCC(=O)N1CCN(CC1)C=2C=C(NC=3SC(C(NC4=C(C)C=CC=C4Cl)=O)=CN3)N=C(C)N2)=O)[C@](C)(C)C)(=O)N5[C@H](C(NCC6=CC=C(C=C6)C7=C(C)N=CS7)=O)C[C@@H](O)C5
Relative Density.	1.335 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 245 mg/mL (241.93 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (4.94 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.9875 mL	4.9374 mL	9.8748 mL	49.3739 mL
5 mM	0.1975 mL	0.9875 mL	1.9750 mL	9.8748 mL
10 mM	0.0987 mL	0.4937 mL	0.9875 mL	4.9374 mL
20 mM	0.0494 mL	0.2469 mL	0.4937 mL	2.4687 mL
50 mM	0.0197 mL	0.0987 mL	0.1975 mL	0.9875 mL
100 mM	0.0099 mL	0.0494 mL	0.0987 mL	0.4937 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc