SHY-867
Based on 1 Customer Validation
SHY-867 is a pan RAS inhibitor. SHY-867 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with EC50 values of 0.5-3 μM. SHY-867 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-867 inhibits the formation of the Ras-GTP activity complex. SHY-867 can be used to the studies of pancreatic cancer and non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity: 99.66%
- CAS No.: 2446484-96-2
- Formula: C26H27N7OS
- Molecular Weight:485.60
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All MEK Isoforms
More
Biological Activity
|
K-Ras WT 2 μM (IC50) |
KRas G12D 2.5 μM (IC50) |
KRas G12C 1.2 μM (IC50) |
KRas Q61H 3 μM (IC50) |
MEK |
ERK1 |
ERK2 |
Akt |
SHY-867 competes with GTP binding to K-Ras WT, the G12D, G12C, and Q61H mutants, as well as Rac-1, Rho-A, Rab5, and Rab35 with IC50s of 2, 2.5, 1.2, 3, 2.5, 3, 0.5 and 0.75 μM[1].
SHY-867 (0.1-1 μM, 72 h) exhibits potent antiproliferative effects in multiple tumor cell lines, including pancreatic cancer (PANC-1, MIA PaCa-2, BxPC3) and non-small cell lung cancer (NCI-H1975, A549, NCI-H1299), with IC50 values ranging from 0.3-1 μM[1].
SHY-867 (0.3-10 μM, 6 h) significantly inhibits the phosphorylation of key signaling molecules induced by EGF in PANC-1, MIA PaCa-2 and NCI-H1975 cells[1].
SHY-867 (1.25-10 μM, 6 h) inhibits Ras-GTP complex formation with an IC50 of 1-3 μM in PANC-1, MIA PaCa-2 and NCI-H1975 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:PANC-1, MIA PaCa-2 and NCI-H1975 cells
-
Concentration:0.3, 0.6, 1.25, 2.5, 5 and 10 μM
-
Incubation Time:6 h
-
Result:Exhibited IC50s on the phosphorylation of MEK and Erk1/2 were approximately 1 μM in PANC-1 and MIA PaCa-2 and 5 μM in NCI-H1975.
Exhibited IC50s of approximately 7 μM in PANC-1 and MIA PaCa-2 and 10 μM in NCI-H1975 for Akt.
Prevented Ras-GTP complex formation with IC50 values in the range of 1 to 3 μM.
Chemical Information
-
CAS No. 2446484-96-2
-
Appearance Solid
-
Molecular Weight 485.60
-
Formula C26H27N7OS
-
Color Off-white to light yellow
-
SMILES
CO[C@H]1CC[C@H](C1)NC2=NC(C3=NC=CN3C)=NC4=C2C(C5=CC=CC=C5)=C(S4)C6=NN(C=C6)C
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
-
Data Sheet (278 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)