2. Protein Tyrosine Kinase/RTK PROTAC
  3. FGFR PROTACs
  4. LC-MB12

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.

For research use only. We do not sell to patients.

LC-MB12 Chemical Structure

LC-MB12 Chemical Structure

CAS No. : 2828438-38-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 657 In-stock
Solution
10 mM * 1 mL in DMSO USD 657 In-stock
Solid
5 mg USD 415 In-stock
10 mg USD 664 In-stock
25 mg USD 1328 In-stock
50 mg USD 2125 In-stock
100 mg USD 3400 In-stock
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Based on 1 publication(s) in Google Scholar

LC-MB12 Related Antibodies

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Description

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].

IC50 & Target

FGFR2

11.8 nM (DC50)

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.

LC-MB12 Related Antibodies

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 (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]

parameter T1/2 Tmax (ng•h/mL) Cmax AUC(0-∞)1/2 Vss (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.
Molecular Weight

899.78

Formula

C43H44Cl2N10O8
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1114 mL 5.5569 mL 11.1138 mL
5 mM 0.2223 mL 1.1114 mL 2.2228 mL
View the Complete Stock Solution Preparation Table

* 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.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LC-MB122828438-38-4FGFRPROTACsFibroblast growth factor receptorKATO IIINCI-H1581SNU-16orally active xenograftantitumorInhibitorinhibitorinhibit

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