LDN-211904 1PC X 5MG (C005B-227934)

General description

A pyrazolo[1,5-a]pyridine derivative that acts as an potent and reversible EphB3 receptor tyrosine kinase inhibitor with an IC₅₀ of 79 nM with good mouse liver microsomal stability and aqueous solubility. Shown to suppress EphB3-induced autophosphorylation of EphB3 receptor at 10 µM in cells. When profiled against a panel of 288 kinases at 5 µM, found to also inhibit most of the Eph (Erythropoietin-producing hepatocellular carcinoma) receptor kinases including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphB1, EphB2, EphB3, EphB4 and other tyrosine kinases, but not EphA6 and EphA7, and is non-inhibitory towards non-RTK kinases screened except for p38α, p38β, and Qik.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Erythropoietin-producing hepatocellular carcinoma (Eph)

Reversible: yes

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Qiao, L., et al. 2011, Bioorg. Med. Chem. Lett.19, 6122

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 444.87. Empirical Formula: C₂₁H₂₁ClN₄O₅. Quality Level: 100. Assay: ≥. 99% (HPLC). form: solid. potency: 79 . nM IC₅₀. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 50 . mg/mL, clear, nearly colorless. shipped in: ambient. storage temp.: 2-8°C. SMILES string: O: C(NC1: CC: CC: C1Cl)C2: CN: C3C: CC(C4CCNCC4): CN32.OC(C(O): O): O. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.

Shipping Information:

Dry Ice Surcharge & Ice Pack Shipments: $40

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UPC:

51172156

Condition:

New

Weight:

1.00 Ounces

HazmatClass:

No

Quantity:

5

Unit of Measurement:

MG

MPN:

428201-5MG

Temperature Control Device:

Yes