Art. -Nr.: HY-149843

LC-MB12

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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.
(Pink: FGFR2 ligand (HY-160013); Blue: Cereblon ligand (HY-W069604); Black: linker (HY-Y1176)).

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Reinheit: 98.10%
CAS. Nr.: 2828438-38-4
Formel: C₄₃H₄₄Cl₂N₁₀O₈
Molecular Weight:899.78

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

LC-MB12 Chemical Structure

CAS. Nr.: 2828438-38-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]. (Pink: FGFR2 ligand (HY-160013); Blue: Cereblon ligand (HY-W069604); Black: linker (HY-Y1176)).

IC₅₀ & Target

FGFR2

11.8 nM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	10.3 nM Compound: LC-MB12	Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR2 assessed as cell growth inhibition measured after 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR2 assessed as cell growth inhibition measured after 72 hrs by celltiter-glo reagent based assay	[PMID: 37220310]
BaF3	IC₅₀	125.2 nM Compound: LC-MB12	Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR1 assessed as cell growth inhibition measured after 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR1 assessed as cell growth inhibition measured after 72 hrs by celltiter-glo reagent based assay	[PMID: 37220310]
BaF3	IC₅₀	139.2 nM Compound: LC-MB12	Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by celltiter-glo reagent based assay	[PMID: 37220310]
BaF3	IC₅₀	>10000 nM Compound: LC-MB12	Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR4 assessed as cell growth inhibition measured after 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR4 assessed as cell growth inhibition measured after 72 hrs by celltiter-glo reagent based assay	[PMID: 37220310]
HEK-293T	IC₅₀	>10000 nM Compound: LC-MB12	Antiproliferative activity against human HEK293T cells assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against human HEK293T cells assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay	[PMID: 37220310]
KATO III stomach cancer cell line	IC₅₀	29.1 nM Compound: LC-MB12	Antiproliferative activity against human KATO III stomach cancer cell line assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against human KATO III stomach cancer cell line assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay	[PMID: 37220310]
MV4-11	IC₅₀	>10000 nM Compound: LC-MB12	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay	[PMID: 37220310]
NCI-H1975	IC₅₀	>10000 nM Compound: LC-MB12	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay	[PMID: 37220310]
NCI-H716	IC₅₀	3.2 nM Compound: LC-MB12	Antiproliferative activity against human NCI-H716 cells assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against human NCI-H716 cells assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay	[PMID: 37220310]
SNU-16	IC₅₀	3.7 nM Compound: LC-MB12	Antiproliferative activity against human SNU-16 cells assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against human SNU-16 cells assessed as reduction in cell viability measured for 72 hrs by celltiter-glo reagent based assay	[PMID: 37220310]

In Vitro

LC-MB12 (0.5-10,000 nM, 3-12 hours) degrades FGFR2 in a time-dependent manner in KATO III, with a DC₅₀ of 11.8 nM.
LC-MB12 (100 nM, 6 hours) degrades FGFR2 to 77% in KATO III and 43% in NCI-H1581^[1].
LC-MB12 (1-10000 nM, 72 hours) inhibits the growth of KATO III, SNU-16, and NCI-H716 significantly with IC₅₀s of 29.1 nM, 3.7 nM and 3.2 nM, respectively, and induces KATO III G0/G1 phase arrest^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

KATO III, SNU-16, NCI-H716
Concentration:

0.5 nM, 1.5 nM, 4.3 nM, 13 nM, 41 nM, 123 nM, 370 nM, 1111 nM, 3333 nM, 10000 nM
Incubation Time:

72 h
Result:

Inhibited cell growth with IC₅₀s value of 29.1 nM (KATO III); 3.7 nM (SNU-16); 3.2 nM (NCI-H716).

Cell Cycle Analysis^[1]

Cell Line:

KATO III
Concentration:

29.1 nM
Incubation Time:

72 h
Result:

Induced G0/G1 cycle arrest.

Immunofluorescence^[1]

Cell Line:

KATO III
Concentration:

100 nM
Incubation Time:

3 h, 6 h
Result:

Promoted FGFR2 was relocated from the cell membrane to intracellular vesicles after treated for 3 or 6 h. Induced receptor internalization and re-localization to the perinuclear section after 6 h treatment.

Western Blot Analysis^[1]

Cell Line:

KATO III, NCI-H1581
Concentration:

0.5 nM, 1.5 nM, 4.3 nM, 13 nM, 41 nM, 123 nM, 370 nM, 1111 nM, 3333 nM, 10000 nM
Incubation Time:

6 h
Result:

Degraded FGFR2 with a DC₅₀ of 11.8 nM and D _max of ~80% after 6 h of treatment.
Showed time-dependent effect on degradation,with a detectable reduction in FGFR2 levels after 3 h of treatment and ~90% degradation after 12 h.
Degraded of FGFR2 in KATO by 77%, and in NCI-H1581 by 43% after 100 nM treatment for 6 h.

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 (C_max: 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]

parameter	T_1/2	T_max (ng•h/mL)	C_max	AUC_(0-∞)1/2	V_ss (h)	CL	F
unit	h	h	ng/mL	h^*ng/mL	mL/kg	mL/h/kg	%
iv (3 mg/kg)	0.97	0.083	655.29	421.61	6233.19	7289.12	/
po (20 mg/kg)	1.47	2.67	82.07	387.27	/	/	13.07

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS. Nr. 2828438-38-4
Appearance Solid
Molecular Weight 899.78
Formel C₄₃H₄₄Cl₂N₁₀O₈
Color Light yellow to yellow
SMILES

O=C(N(C)C1=CC(NC2=CC=C(N3CCN(CC3)C(C4CCN(CC4)C5=CC=C6C(N(C7C(NC(CC7)=O)=O)C(C6=C5)=O)=O)=O)C=C2)=NC=N1)NC8=C(Cl)C(OC)=CC(OC)=C8Cl
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 130 mg/mL (144.48 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1114 mL

5.5569 mL

11.1138 mL

5 mM

0.2223 mL

1.1114 mL

2.2228 mL

10 mM

0.1111 mL

0.5557 mL

1.1114 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1114 mL	5.5569 mL	11.1138 mL	27.7846 mL
	5 mM	0.2223 mL	1.1114 mL	2.2228 mL	5.5569 mL
	10 mM	0.1111 mL	0.5557 mL	1.1114 mL	2.7785 mL
	15 mM	0.0741 mL	0.3705 mL	0.7409 mL	1.8523 mL
	20 mM	0.0556 mL	0.2778 mL	0.5557 mL	1.3892 mL
	25 mM	0.0445 mL	0.2223 mL	0.4446 mL	1.1114 mL
	30 mM	0.0370 mL	0.1852 mL	0.3705 mL	0.9262 mL
	40 mM	0.0278 mL	0.1389 mL	0.2778 mL	0.6946 mL
	50 mM	0.0222 mL	0.1111 mL	0.2223 mL	0.5557 mL
	60 mM	0.0185 mL	0.0926 mL	0.1852 mL	0.4631 mL
	80 mM	0.0139 mL	0.0695 mL	0.1389 mL	0.3473 mL
	100 mM	0.0111 mL	0.0556 mL	0.1111 mL	0.2778 mL

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LC-MB12

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

PROTAC Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LC-MB12

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

PROTAC Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LC-MB12 Related Classifications

HY-149843 Related Classifications