2. Protein Tyrosine Kinase/RTK
  3. Ephrin Receptor
  4. LDN-211904 oxalate

LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC.

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LDN-211904 oxalate Chemical Structure

LDN-211904 oxalate Chemical Structure

CAS No. : 1198408-78-4

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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Based on 1 publication(s) in Google Scholar

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LDN-211904 oxalate Related Antibodies

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Description

LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC[1][2].

IC50 & Target

IC50: 0.079 µM (EphB3)[1]
In Vitro

LDN-211904 (20 μM; 24 h) oxalate induces apoptosis by increasing c-PARP in SW48 resistant cells[2].
LDN-211904 (20 μM; 4-20 h) oxalate decreases the levels of p-STAT3, GLI-1, SOX2 and Vimentin in SW48 resistant cells[2].

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

LDN-211904 oxalate Related Antibodies

Apoptosis Analysis[2]

Cell Line: SW48 and SW48 Cetuximab-resistant (SW48R) cells
Concentration: 20 μM
Incubation Time: 24 h
Result: Induced apoptosis by increasing c-PARP.

Western Blot Analysis[2]

Cell Line: SW48 and SW48 Cetuximab-resistant (SW48R) cells
Concentration: 20 μM
Incubation Time: 4 h, 8 h, 20 h
Result: The levels of p-STAT3, GLI-1, SOX2 and Vimentin in SW48 resistant cells were decreased.
In Vivo

LDN-211904 (0.1 mg/kg; i.p.; three times a week; for 21 days) oxalate inhibits and overcomes Cetuximab (HY-P9905) resistance in vivo[2].

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

Animal Model: Four-week-old female BALB/c nude mice were implanted subcutaneously SW48 cells[2]
Dosage: 0.1 mg/kg
Administration: i.p.; three times a week; for 21 days
Result: Inhibited tumor growth.
Molecular Weight

444.87

Formula

C21H21ClN4O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(O)=O)O.O=C(C1=CN=C2C=CC(C3CCNCC3)=CN21)NC4=C(Cl)C=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Purity: ≥99.0%

SDS (251 KB)

COA (249 KB)

Handling Instructions (2659 KB)
References
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LDN-211904 oxalate Related Classifications

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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:

LDN-2119041198408-78-4LDN211904LDN 211904Ephrin Receptormetabolic stabilitySW48R tumor cellsCSC stemnessCRCInhibitorinhibitorinhibit

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