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ADTL-EI1712

Catalog No. T38377 CAS 2414916-45-1

Synonyms: ADTL-EI1712

ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC50s = 40.43 and 64.5 nM, respectively).1It reduces ERK1 and ERK5 activity by 93.5% and 89.4%, respectively, but also inhibits ERK2 activity by 92.7%, in a panel of 100 kinases at 1 μM. ADTL-EI1712 inhibits proliferation of HL-60 and MKN74, but not HeLa, cancer cells (IC50s = 1.26, 2.55, and <50 μM, respectively). It reduces tumor growth and intratumor phosphorylation of ERK1/2 and ERK5 in an MKN74 mouse xenograft model when administered at a dose of 50 mg/kg per day.

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ADTL-EI1712, CAS 2414916-45-1

Pack Size	Availability	Price/USD
1 mg	35 days	$ 155.00
5 mg	35 days	$ 294.00
10 mg	35 days	$ 528.00
25 mg	35 days	$ 1,120.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description

ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC50s = 40.43 and 64.5 nM, respectively).1It reduces ERK1 and ERK5 activity by 93.5% and 89.4%, respectively, but also inhibits ERK2 activity by 92.7%, in a panel of 100 kinases at 1 μM. ADTL-EI1712 inhibits proliferation of HL-60 and MKN74, but not HeLa, cancer cells (IC50s = 1.26, 2.55, and >50 μM, respectively). It reduces tumor growth and intratumor phosphorylation of ERK1/2 and ERK5 in an MKN74 mouse xenograft model when administered at a dose of 50 mg/kg per day.

Synonyms	ADTL-EI1712
Molecular Weight	505.44
Formula	C22H18Cl2N4O2S2
CAS No.	2414916-45-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMF: 1 mg/mL

DMSO: 1 mg/mL

DMSO:PBS (pH 7.2) (1:3): 0.25 mg/mL

References and Literature

1. Wang, G., Zhao, Y., Liu, Y., et al.Discovery of a novel dual-target inhibitor of ERK1 and ERK5 that induces regulated cell death to overcome compensatory mechanism in specific tumor typesJ. Med. Chem.63(8)3976-3995(2020)

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

ADTL-EI1712 2414916-45-1 ADTLEI1712 ADTL-EI-1712 ADTL EI1712 ADTL-EI 1712 inhibitor inhibit

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