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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $137 | In Stock | In Stock | |
| 5 mg | $342 | In Stock | In Stock | |
| 10 mg | $549 | In Stock | In Stock | |
| 25 mg | $1,080 | In Stock | In Stock | |
| 50 mg | $1,760 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $543 | In Stock | In Stock |
| 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] |
| Synonyms | LCMB12 |
| Molecular Weight | 899.78 |
| Formula | C43H44Cl2N10O8 |
| Cas No. | 2828438-38-4 |
| Smiles | O=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 | keep 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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
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
and mix thoroughly until a homogeneous solution is obtained.
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