APS-2-79|cas 2002381-25-9|DC Chemicals

Cas No.:	2002381-25-9
Chemical Name:	6,7-Dimethoxy-~{n}-(2-Methyl-4-Phenoxy-Phenyl)quinazolin-4-Amine
Synonyms:	APS-2-79;APS 2-79;6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine;6,7-Dimethoxy-~{n}-(2-Methyl-4-Phenoxy-Phenyl)quinazolin-4-Amine;BDBM429286;BCP24938;US10548897, Compound 21;Q27456559;COC=1C=C2C(=NC=NC2=CC=1OC)NC1=C(C=C(C=C1)OC1=CC=CC=C1)C;6U7
SMILES:	O(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C(=C(C([H])([H])[H])C=1[H])N([H])C1C2=C([H])C(=C(C([H])=C2N=C([H])N=1)OC([H])([H])[H])OC([H])([H])[H]
Formula:	C₂₃H₂₁N₃O₃
M.Wt:	387.4311
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

APS-2-79 behaves as a kinase suppressor of Ras (KSR)-dependent antagonist of RAF-mediated MEK phosphorylation. APS-2-79 binds directly to KSR2 within the KSR2-MEK1 complex with an IC 50 of 120±23 nM for KSR2.

In Vitro:

APS-2-79 (1 μM) shifts the cell viability dose response to Trametinib in Ras-mutant cell lines HCT-116 and A549, but not BRAF mutant cell lines SK-MEL-239 and A375. Although the cellular effects of APS-2-79 alone are modest, combination analysis over full concentration matrices reveal that kinase suppressor of Ras (KSR)-inactive state (KSRi) synergizes with Trametinib, and other MEK inhibitors, specifically in KRAS mutant cell lines. APS-3-77, and additional control compounds, do not demonstrate Ras-mutant-specific synergy, supporting the hypothesis that the enhanced activity of Trametinib when combined with APS-2-79 depends on co-modulation of KSR[1].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC7488	RO4987655	RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.
DC8473	Vacquinol-1	Vacquinol-1 is an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells.
DC7243	U0126	U0126-EtOH(U-0126) is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD098059.
DC1099	Trametinib	Trametinib is a highly specific and potent MEK1 and MEK2 inhibitor with IC50 of 0.92 nM and 1.8 nM, respectively.
DC7308	TAK-733	TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.
DC7808	Refametinib (BAY86-9766)	Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.
DC1056	PD0325901 (Mirdametinib)	PD0325901 (PD325901) is selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM.
DC5100	PD 98059	PD 98059 is a selective inhibitor of MEK and blocker of MAPK
DC7723	OTS964， OTS 964	OTS964 is a novel TOPK(T–lymphokine-activated killer cell–originated protein kinase) inhibitor.
DC4177	Cobimetinib(GDC-0973; XL518)	GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase, also known as MEK, a serine/threonine kinase that is a component of the RAS/RAF/MEK/ERK pathway.