DEL-22379 free base · Synonyms: DEL 22379 · DEL22379

DEL-22379 is an ERK dimerization Inhibitor.

For research use only. Not for human or veterinary use.

Target ERK Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

DEL-22379 structure

CAS No.: 181223-80-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 480.00	BP-01932-250mg	In stock	Get quote
500 mg	USD 720.00	BP-01932-500mg	In stock	Get quote
1 g	USD 1,120.00	BP-01932-1g	In stock	Get quote
5 g	Inquire	BP-01932-5g	Inquire	Inquire

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Description

DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.

Biological activity

In Vitro DEL-22379 is an ERK dimerization inhibitor. DEL-22379 abolishes EGF-induced co-immunoprecipitation of ectopic ERK2 molecules tagged with hemagglutinin (HA) or FLAG epitopes, with an estimated half-maximal inhibitory concentration (IC50) of ~0.5 μM. DEL-22379 inhibits growth of tumor cells harboring RAS-ERK pathway oncogenes. The biological effects of DEL-22379 are investigated on tumor cells in culture. The cytostatic effects of DEL-22379 are compared to those of the MEK inhibitor PD-0325901 and the ERK kinase inhibitor SCH-772984, as reflected by their half-maximal growth inhibitory concentrations (GI50). Cell lines harboring mutant BRAF are the most sensitive to the three compounds. In comparison, wild-type (WT) cell lines for BRAF and RAS are the most resistant, and RAS mutant cells exhibit a range of sensitivities. In cells showing different oncogenic genotypes, distinct sensitivity to DEL-22379 can not be attributed to variations on its effects on dimerization, because DEL-22379 displays similar dimerization- and cytoplasmic signaling-inhibitory dose responses (IC50 of 150-400 nM) regardless of the genotype. In Vivo To test DEL-22379 antitumor effects, some of the aforementioned cell lines are xenografted into nude mice, and tumor growth is monitored after intra-peritoneal administration of DEL-22379 at 15 mg/kg. At such a dose, inhibition of ERK dimerization is evident in liver extracts and in xenografted tumors. DEL-22379 markedly inhibits tumor progression for A375 cells (BRAF mutant).

Identifiers

SMILES: COC1=CC2=C(NC=C2\C=C2/C(=O)NC3=C2C=C(NC(=O)CCN2CCCCC2)C=C3)C=C1
InChIKey: INQUULPXCZAKMS-XKZIYDEJSA-N

Specifications

MW (average): 444.5255
Formula: C₂₆H₂₈N₄O₃
CAS No.: 181223-80-3
Physical state: Solid
Color: Yellow to orange
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Herrero A, et al. Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes. Cancer Cell. 2015 Aug 10;28(2):170-82.

Same target

Search ERK

Same research area

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