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2828438-38-4

2828438-38-4 Structure

2828438-38-4 Structure
IdentificationBack Directory
[Name]

LC-MB12
[CAS]

2828438-38-4
[Synonyms]

LC-MB12
[Molecular Formula]

C43H44Cl2N10O8
[MOL File]

2828438-38-4.mol
[Molecular Weight]

899.78
Chemical PropertiesBack Directory
[Boiling point ]

1125.6±65.0 °C(predicted)
[density ]

1.481±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
[form ]

Solid
[pka]

10.83±0.40(predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Uses]

LC-MB12 is an orally active PROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM. LC-MB12 contains BGJ398 (a FGFR2 inhibitor), PROTAC linker and CRBN.LC-MB12 inhibits FGFR2 signaling in gastric cancer cells and has anti-tumor activity[1].
[in vivo]

LC-MB12 (20 mg/kg/day, p.o., 15 days) inhibits tumor growth to 63.1% in SNU-16 xenograft models of nude mice[1].
LC-MB12 (20 mg/kg, p.o.) shows fast absorption (Cmax: 2.6 h) and orally bioavailable (F: 13%) in mice[1].
LC-MB12 (20 mg/kg, p.o., 30 days) is well tolerated and has no apparent hepatotoxicity or nephrotoxicity in mice[1].

In Vivo PK Properties of LC-MB12[1]

parameterT1/2Tmax (ng?h/mL)CmaxAUC(0-∞)1/2Vss (h)CL F
unithhng/mLh*ng/mLmL/kgmL/h/kg%
iv (3 mg/kg)0.970.083655.29421.616233.197289.12/
po (20 mg/kg)1.472.6782.07387.27//13.07
Animal Model:SNU-16 xenografted in BALB/c-nu mice[1].
Dosage:20 mg/kg/day
Administration:oral administration (p.o.) 15 days
Result:Achieved 63.1% tumor growth inhibition innocuously.
Inhibited FGFR phosphorylation and total FGFR2 protein and decreased phosphorylation levels of downstream pPLCγ and ERK1/2.
[IC 50]

FGFR2: 11.8 nM (DC50)
[References]

[1] Ma L, et al. Discovery of a Selective and Orally Bioavailable FGFR2 Degrader for Treating Gastric Cancer. J Med Chem. 2023 Jun 8;66(11):7438-7453. DOI:10.1021/acs.jmedchem.3c00150
2828438-38-4 suppliers list
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Company Name: TargetMol Chemicals Inc.  
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Website: https://www.targetmol.cn/
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