APS-2-79
- Product Name
- APS-2-79
- CAS No.
- 2002381-31-7
- Chemical Name
- APS-2-79
- Synonyms
- CS-2444;APS-2-79;APS 2 79;APS279;APS-279;APS-2-79 (hydrochloride);APS-2-79 hydrochloride >=98% (HPLC);APS-2-79 hydrochloride, 10 mM in DMSO;6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine hydrochloride;MAP2K,MAPKK,Inhibitor,Mitogen-activated protein kinase kinase,APS 2 79 hydrochloride,APS279 hydrochloride,inhibit,MEK
- CBNumber
- CB43145564
- Molecular Formula
- C23H22ClN3O3
- Formula Weight
- 423.9
- MOL File
- 2002381-31-7.mol
APS-2-79 Property
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- A crystalline solid
- color
- white to beige
Safety
- HS Code
- 2933599590
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H302Harmful if swallowed
H361Suspected of damaging fertility or the unborn child
H372Causes damage to organs through prolonged or repeated exposure
H410Very toxic to aquatic life with long lasting effects
- Precautionary statements
-
P201Obtain special instructions before use.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P330+P331IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
N-Bromosuccinimide Price
- Product number
- 22137
- Product name
- APS-2-79 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $33
- Updated
- 2024/03/01
- Product number
- 22137
- Product name
- APS-2-79 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $89
- Updated
- 2024/03/01
- Product number
- 22137
- Product name
- APS-2-79 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $160
- Updated
- 2024/03/01
- Product number
- 22137
- Product name
- APS-2-79 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 25mg
- Price
- $356
- Updated
- 2024/03/01
- Product number
- B7820
- Product name
- APS-2-79
- Packaging
- 5mg
- Price
- $122
- Updated
- 2021/12/16
APS-2-79 Chemical Properties,Usage,Production
Description
APS-2-79 is an inhibitor of MAPK signaling dependent on kinase suppressor of Ras (KSR). It inhibits ATPbiotin binding to KSR2 in KSR2-MEK1 complexes (IC50 = 120 nM), stabilizes KSR2 in an inactive state, and reduces interactions between B-RAF and KSR2-MEK1 complexes. APS-2-79 (5 μM) inhibits KSR-stimulated phosphorylation of MEK and ERK in HEK293H cells. It enhances the efficacy of the MEK inhibitor trametinib , further reducing cell viability in HCT116 and A549 cell lines containing K-Ras mutations, but not B-RAF mutant SK-MEL-239 and A375 cell lines, when used at a concentration of 1 μM.
Uses
APS-2-79 is a modulator of KSR-dependent MAPK signaling, antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation as well as the activation of KSR-bound MEK (mitogen-activated protein kinase).
in vitro
aps-2-79 was found to be able to suppress ksr-stimulated mek and erk phosphorylation. this mapk signalling suppression caused by aps-2-79 was dependent on direct targeting of ksr as an active site mutant, which had been demonstrated to stimulate ksr-based mapk outputs independent of atp-binding, which could significantly diminish the activity of aps-2-79. moreover, the ksr-stimulated mek phosphorylation caused by raf was reduced by the addition of aps-2-79 markedly. in addition, aps-2-79 was no effetive when ksr was absent or when the ksr2(a690f) mutant was used for in vitro assays, indicating that the activity of aps-2-79 was from direct targeting of ksr. however, aps-2-79 was found to lack direct activity against the highly homologous active raf family kinases, such as recombinant braf and craf, or cellular braf(v600e) [1].
IC 50
120 nm
References
[1] dhawan ns, scopton ap, dar ac. small molecule stabilization of the ksr inactive state antagonizes oncogenic ras signalling. nature. 2016 sep 1;537(7618):112-116.
APS-2-79 Preparation Products And Raw materials
Raw materials
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