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I-138

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Purity:99.41%

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COA HPLC HNMR

I-138

Catalog No. T73560Cas No. 2098211-50-6

I-138 is an orally active and potent reversible inhibitor of USP1-UAF1.I-138 induces mono-ubiquitination of FANCD2 and PCNA and inhibits USP1 auto-cleavage in cells.

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Pack Size	Price	Availability
1 mg	$198	In Stock
2 mg	$268	In Stock
5 mg	$388	In Stock
10 mg	$629	In Stock
25 mg	$1,180	In Stock
50 mg	$1,790	In Stock
100 mg	$2,320	In Stock
1 mL x 10 mM (in DMSO)	$448	In Stock

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Product Introduction

Bioactivity

Description	I-138 is an orally active and potent reversible inhibitor of USP1-UAF1.I-138 induces mono-ubiquitination of FANCD2 and PCNA and inhibits USP1 auto-cleavage in cells.
In vitro	I-138 (0.5 μM; 4 hours) eliminates USP1 autodeubiquitination in HAP-1 USP1 WT and knockout cells, induces monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells, and dose-dependently (0.01-10 μM; 10 days) inhibits the viability of MDA-MB-436 cells without affecting HCC1954 cells[1].
In vivo	I-138 (50 mg/kg/day; oral administration; for 41 days) shows USP1 inhibition and moderate antitumor activity in mice with MDA-MB-436 tumors. However, combining I-138 with the PARP inhibitor Niraparib is more effective at inhibiting BRCA1/2 mutant tumors in vivo[1].

Chemical Properties

Molecular Weight	492.5
Formula	C26H23F3N6O
Cas No.	2098211-50-6

Storage & Solubility Information

Storage

store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (162.44 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0305 mL	10.1523 mL	20.3046 mL	101.5228 mL
5 mM	0.4061 mL	2.0305 mL	4.0609 mL	20.3046 mL
10 mM	0.2030 mL	1.0152 mL	2.0305 mL	10.1523 mL
20 mM	0.1015 mL	0.5076 mL	1.0152 mL	5.0761 mL
50 mM	0.0406 mL	0.2030 mL	0.4061 mL	2.0305 mL
100 mM	0.0203 mL	0.1015 mL	0.2030 mL	1.0152 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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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

I-138

I-138

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