[CAS NO. 2376047-73-1] SIAIS178
PRODUCTS SPECIFICATIONS [2376047-73-1]
DESCRIPTION [2376047-73-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1012.68 |
| Molecular Formula | C50H62ClN11O6S2 |
| SMILES | O=C(N1CCN(C2=NC(C)=NC(NC3=NC=C(C(NC4=C(C=CC=C4Cl)C)=O)S3)=C2)CC1)CCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@@H](O)C5)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O |
Summary
IC50 & Target
|
VHL
|
Bcr-Abl 24 nM (IC 50 ) |
In Vitro
SIAIS178 (1-100 nM; for 16 hours) significantly reduces the BCR-ABL protein levels in a concentration dependent manner. SIAIS178 significantly inhibits the phosphorylation of BCR-ABL and the substrates STAT5
[1]
.
SIAIS178 (1, 10, 100, 1000 nM) exerts significant antiproliferative activity in BCR-ABL driven CML cell lines. SIAIS178 retains potency and selectivity against the BCR-ABL driven cell lines
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | K562 cells |
| Concentration: | 1, 3, 10, 30, 100 nM |
| Incubation Time: | 16 hours |
| Result: | Significantly reduced the BCR-ABL protein levels in a concentration dependent manner. |
In Vivo
SIAIS178 (ip; 5, 15, and 45 mg/kg; 12 days) attenuates tumor progression in a dose-dependent manner, as determined by serial volumetric measurement
[1]
.
SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T
1/2
of 3.82 and 12.35 hours and C
max
of 1165.2 nM and 30 nM for iv and ip, respectively
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | NOD/SCID mice with termed K562-Luc [1] |
| Dosage: | 5, 15, and 45 mg/kg |
| Administration: | Ip; 12 days |
| Result: | Attenuated tumor progression in a dose-dependent manner, as determined by serial volumetric measurement. |
| Animal Model: | Female Wistar rats [1] |
| Dosage: | 2 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Iv or ip; 24 hours |
| Result: | Had T 1/2 of 3.82 and 12.35 hours and C max of 1165.2 nM and 30 nM for iv and ip, respectively. |
Appearance
Solid
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 |
Solvent & Solubility
DMSO : 300 mg/mL ( 296.24 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.9875 mL | 4.9374 mL | 9.8748 mL |
| 5 mM | 0.1975 mL | 0.9875 mL | 1.9750 mL |
| 10 mM | 0.0987 mL | 0.4937 mL | 0.9875 mL |
-
1.