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KSQ-4279

Name: KSQ-4279
Brand: TargetMol
SKU: T60039
Price: 158 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: USP1-IN-1) Copy Product Info

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Synonyms: USP1-IN-1

Catalog No. T60039 Copy Product Info

Purity: 99.98%

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KSQ-4279 (USP1-IN-1) is a dual USP1/PARP inhibitor, a potent and selective PARP inhibitor with anti-cancer activity, used for research in non-small cell lung cancer and various other cancers.

Cas No. 2446480-97-1

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Pack Size	Price	USA Stock	Global Stock
1 mg	$158	In Stock	In Stock
5 mg	$396	In Stock	In Stock
10 mg	$589	In Stock	In Stock
25 mg	$943	In Stock	In Stock
50 mg	$1,280	In Stock	In Stock
100 mg	$1,720	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.98%

Appearance:Solid

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	KSQ-4279 (USP1-IN-1) is a dual USP1/PARP inhibitor, a potent and selective PARP inhibitor with anti-cancer activity, used for research in non-small cell lung cancer and various other cancers.
Targets & IC50	USP1:21.1 nM
In vitro	Methods: MTT assay was used in MDR cells overexpressing ABCB1, ABCG2, or ABCC1 (KBv200, MCF7/adr, S1-MI-80, H460/MX20, HL60/adr and corresponding stable transfectants), incubated with 2.5, 5, 10 μmol/L KSQ-4279 for 72 h. Results: KSQ-4279 significantly enhanced the cytotoxicity of multiple chemotherapeutic drugs against MDR cells, with negligible cytotoxicity of its own. [1]
In vivo	Methods: In BALB/c nude mouse KBv200, S1-MI-80, and HL60/adr xenograft models, KSQ-4279 (30 mg/kg, gavage, every two days, dissolved in DMSO/PEG300/Tween-80/normal saline) was combined with paclitaxel (15 mg/kg), topotecan (2 mg/kg), or doxorubicin (3 mg/kg) by intraperitoneal injection. Results: The combination group significantly inhibited tumor growth without causing body weight loss. [1] Methods: In BALB/c nude mouse or NOD/SCID IL2Rγnull mouse subcutaneous and orthotopic PDX models, KSQ-4279 was administered orally by gavage at 10–300 mg/kg once daily (dissolved in 0.5% HPMC/0.1% Tween 80). Results: Monotherapy inhibited growth of some BRCA-mutant tumors; when combined with olaparib or AZD5305, sustained tumor regression was achieved in various PARP inhibitor-resistant models with good tolerability. [2]
Synonyms	USP1-IN-1

Chemical Properties

Molecular Weight	534.54
Formula	C₂₇H₂₅F₃N₈O
Cas No.	2446480-97-1
Smiles	COc1ncnc(C2CC2)c1-c1ncc2cnn(Cc3ccc(cc3)-c3nc(cn3C(C)C)C(F)(F)F)c2n1
Relative Density.	1.47 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 255 mg/mL (477.05 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.17 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	1.8708 mL	9.3538 mL	18.7077 mL	93.5384 mL
5 mM	0.3742 mL	1.8708 mL	3.7415 mL	18.7077 mL
10 mM	0.1871 mL	0.9354 mL	1.8708 mL	9.3538 mL
20 mM	0.0935 mL	0.4677 mL	0.9354 mL	4.6769 mL
50 mM	0.0374 mL	0.1871 mL	0.3742 mL	1.8708 mL
100 mM	0.0187 mL	0.0935 mL	0.1871 mL	0.9354 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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.