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LC-MB12

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Catalog No. T86805Cas No. 2828438-38-4
Alias LCMB12

LC-MB12 is an orally active, selective and potent PROTAC FGFR2 complex that degrades FGFR2.LC-MB12 has antiproliferative and antitumor activity.LC-MB12 is used in the study of gastric cancer because of its inhibition of FGFR2 signaling.LC-MB12 has been shown to have antiproliferative and antitumor activity.LC-MB12 has been shown to have antiproliferative and antitumor activity.

LC-MB12

LC-MB12

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Purity: 99.16%
Catalog No. T86805Alias LCMB12Cas No. 2828438-38-4
LC-MB12 is an orally active, selective and potent PROTAC FGFR2 complex that degrades FGFR2.LC-MB12 has antiproliferative and antitumor activity.LC-MB12 is used in the study of gastric cancer because of its inhibition of FGFR2 signaling.LC-MB12 has been shown to have antiproliferative and antitumor activity.LC-MB12 has been shown to have antiproliferative and antitumor activity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$137In StockIn Stock
5 mg$342In StockIn Stock
10 mg$549In StockIn Stock
25 mg$1,080In StockIn Stock
50 mg$1,760In StockIn Stock
1 mL x 10 mM (in DMSO)$543In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.16%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
LC-MB12 is an orally active, selective and potent PROTAC FGFR2 complex that degrades FGFR2.LC-MB12 has antiproliferative and antitumor activity.LC-MB12 is used in the study of gastric cancer because of its inhibition of FGFR2 signaling.LC-MB12 has been shown to have antiproliferative and antitumor activity.LC-MB12 has been shown to have antiproliferative and antitumor activity.
Targets&IC50
KATO III cells:29.1 nM, NCI-H716 cells:3.2 nM, FGFR2:11.8 nM (DC50), SNU-16 cells:3.7 nM
In vitro
0.5-10000 nM LC-MB12, FGFR2 was degraded in KATO III in a time-dependent manner over 3-12 hours, DC50=11.8 nM. [1]
100 nM LC-MB12 treatment for 6 hours resulted in 77% degradation of FGFR2 in KATO III and 43% degradation in NCI-H1581. [1]
1-10000 nM LC-MB12 treatment for 72 h significantly inhibited the growth of KATO III, SNU-16, and NCI-H716 with IC50=29.1 nM (KATO III), IC50=3.7 nM (SNU-16), and IC50=3.2 nM (NCI-H716), respectively, and induced KATO III G0 /G1 phase block. [1]
In vivo
Oral administration of 20 mg/kg LC-MB12 was rapidly absorbed in mice (Cmax: 2.6 h) with oral bioavailability (F: 13%). Oral administration for 30 days was well tolerated and showed no significant hepatotoxicity or nephrotoxicity in mice. [1]
20 mg/kg/day LC-MB12 administered orally for 15 days inhibited tumor growth by 63.1% in the SNU-16 nude mouse xenograft model. [1]
SynonymsLCMB12
Chemical Properties
Molecular Weight899.78
FormulaC43H44Cl2N10O8
Cas No.2828438-38-4
SmilesO=C(NC=1C(Cl)=C(OC)C=C(OC)C1Cl)N(C=2N=CN=C(C2)NC3=CC=C(C=C3)N4CCN(C(=O)C5CCN(C6=CC=C7C(=O)N(C(=O)C7=C6)C8C(=O)NC(=O)CC8)CC5)CC4)C
Storage & Solubility Information
Storagekeep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 120 mg/mL(133.37 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.1114 mL5.5569 mL11.1138 mL55.5691 mL
5 mM0.2223 mL1.1114 mL2.2228 mL11.1138 mL
10 mM0.1111 mL0.5557 mL1.1114 mL5.5569 mL
20 mM0.0556 mL0.2778 mL0.5557 mL2.7785 mL
50 mM0.0222 mL0.1111 mL0.2223 mL1.1114 mL
100 mM0.0111 mL0.0556 mL0.1111 mL0.5557 mL

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TargetMol | Animal experiments 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.
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Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

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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.
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