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);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
- Molecular Weight:
- 423.9
- MDL Number:
- MFCD30536203
- MOL File:
- 2002381-31-7.mol
SAFETY
Risk and Safety Statements
| Symbol(GHS) |    GHS07,GHS08,GHS09 |
|---|---|
| Signal word | Danger |
| Hazard statements | H302-H361-H372-H410 |
| Precautionary statements | P201-P264-P280-P301+P330+P331-P312 |
| HS Code | 2933599590 |
APS-2-79 price More Price(15)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 22137 | APS-2-79 (hydrochloride) ≥95% | 2002381-31-7 | 1mg | $33 | 2024-03-01 | Buy |
| Cayman Chemical | 22137 | APS-2-79 (hydrochloride) ≥95% | 2002381-31-7 | 5mg | $89 | 2024-03-01 | Buy |
| Cayman Chemical | 22137 | APS-2-79 (hydrochloride) ≥95% | 2002381-31-7 | 10mg | $160 | 2024-03-01 | Buy |
| Cayman Chemical | 22137 | APS-2-79 (hydrochloride) ≥95% | 2002381-31-7 | 25mg | $356 | 2024-03-01 | Buy |
| ApexBio Technology | B7820 | APS-2-79 | 2002381-31-7 | 5mg | $122 | 2021-12-16 | Buy |
APS-2-79 Chemical Properties,Uses,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
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 4664 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
| ChemShuttle, Inc. | 0510-83588313-802 18800520310; | sales@chemshuttle.com | China | 2968 | 62 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4153 | 55 | |
| ATK CHEMICAL COMPANY LIMITED | 3429815786 13301662590 | sales@atkchemical.com | China | 10004 | 55 |