[CAS NO. 2443816-41-7] SEL120-34A monohydrochloride
PRODUCTS SPECIFICATIONS [2443816-41-7]
DESCRIPTION [2443816-41-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 450.60 |
| Molecular Formula | C15H19Br2ClN4 |
| SMILES | CC1=C2C3=C(C(Br)=C1Br)CCCN3C(N4CCNCC4)=N2.Cl |
3 Publications Citing Use of MCE
Summary
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC 50 s of 4.4 nM and 10.4 nM, respectively, with a K d of 3 nM for CDK8 . SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC 50 =1070 nM), but shows no obvious activity against CDK1 , 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726 [1] . Has anti-tumor activity [1] .
IC50 & Target
|
CDK8/CycC 4.4 nM (IC 50 ) |
CDK19/CycC 10.4 nM (IC 50 ) |
CDK9/cycT 1070 nM (IC 50 ) |
In Vitro
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC
50
s of 4.4 nM and 10.4 nM, respectively, with a K
d
of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC
50
=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7
[1]
.
SEL120-34A (1.6 nM-5 μM) inhibits the growth of STAT5 S726 positive KG-1 AML cells, but is not cytotoxic to S726 negative MOLM13 AML cells
[1]
.
SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726, decreases IRF9 and STAT1 mRNA expression and mitogen-induced IER expression
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SEL120-34A monohydrochloride (30, 60 mg/kg, p.o. once every day) inhibits growth of AML tumors in a dose-dependent manner in SCID mice after treatment for 17 days [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 50 mg/mL ( 110.96 mM ; Need ultrasonic)
DMSO : 16.67 mg/mL ( 37.00 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2193 mL | 11.0963 mL | 22.1926 mL |
| 5 mM | 0.4439 mL | 2.2193 mL | 4.4385 mL |
| 10 mM | 0.2219 mL | 1.1096 mL | 2.2193 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 14.29 mg/mL (31.71 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.67 mg/mL (3.71 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1.67 mg/mL (3.71 mM); Clear solution
