[CAS NO. 2226735-55-1] GSK547
PRODUCTS SPECIFICATIONS [2226735-55-1]
DESCRIPTION [2226735-55-1]
Overview
| MDL | MFCD32062767 |
|---|---|
| Molecular Weight | 396.39 |
| Molecular Formula | C20H18F2N6O |
| SMILES | N#CC1=NC=NC(N2CCC(C(N3N=CC[C@H]3C4=CC(F)=CC(F)=C4)=O)CC2)=C1 |
Summary
IC50 & Target
RIP1 [1]
In Vitro
GSK547 (0.1-100000 nM; 24 hours) pretreats L929 cells with recombinant TNFα and zVAD at various doses for 30 min, then cell death is induced with an IC
50
of 32 nM after 24 hours
[1]
.
GSK547 up-regulates STAT1 signaling in bone marrow-derived macrophages (BMDM)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | L929 cells (Mouse L-cells NCTC 929) |
| Concentration: | 0.1 nM; 10 nM; 1000 nM; 100000 nM |
| Incubation Time: | 24 hours |
| Result: | Reduced viability of L929 cells after co-treatment with TNFα and zVAD with an IC 50 of 32 nM. |
Western Blot Analysis [1]
| Cell Line: | Bone marrow-derived macrophages (BMDM) |
| Concentration: | |
| Incubation Time: | 30 minutes |
| Result: | Up-regulated STAT1 signaling in BMDM. |
In Vivo
GSK547 (GSK′547; RIP1i) robustly targets RIP1 in vivo. RIP1 inhibition results in immunogenic macrophage differentiation in pancreatic cancer, leading to adaptive immune activation and tumor protection for pancreatic ductal adenocarcinoma (PDA)
[1]
.
GSK547 (100 mg/kg/day; fed via food-based dosing; 15-50 days) reduces tumor burden and extends survival compared with mice treated with controls or Nec-1s
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | The wild-type (WT) mice orthotopically implanted with Pdx1 Cre ; Kras G12D ; Trp53 R172H (KPC)-derived tumor cells [1] |
| Dosage: | ~100 mg/kg |
| Administration: | Fed via food-based dosing, daily, 15-50 days |
| Result: | Reduced tumor burden and extended survival. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 250 mg/mL ( 630.69 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5228 mL | 12.6138 mL | 25.2277 mL |
| 5 mM | 0.5046 mL | 2.5228 mL | 5.0455 mL |
| 10 mM | 0.2523 mL | 1.2614 mL | 2.5228 mL |
-
1.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution