[CAS NO. 2079069-01-3] CaseinKinaseinhibitorA86
PRODUCTS SPECIFICATIONS [2079069-01-3]
DESCRIPTION [2079069-01-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 344.43 |
| Molecular Formula | C18H25FN6 |
| SMILES | N[C@H]1CC[C@H](NC2=NC=C(F)C(C3=C(CC4CC4)N(C)N=C3)=N2)CC1 |
Summary
Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb) . Casein Kinase inhibitor A861 induces leukemia cell apoptosis , and has potent anti-leukemic activities [1] .
IC50 & Target
|
CKIα
|
CDK7 0.31 nM (Kd) |
CDK9 5.4 nM (Kd) |
In Vitro
Casein Kinase inhibitor A86 is highly effective in inducing leukemia cell apoptosis at 160 nM or lower, mostly in correlation to their capacity to stabilize p53
[1]
.
Casein Kinase inhibitor A86 (0.08-2 μM; 6.5 hours) abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. Casein Kinase inhibitor A86 induces a marked reduction in mRNA expression of MYC and MDM2, yet upregulates the expression of the Wnt targets AXIN2 and CCND1 (Cyclin D1)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | MV4-11 cells |
| Concentration: | 0.08 μM, 0.6 μM, 2 μM |
| Incubation Time: | 6.5 hours |
| Result: | Abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. |
In Vivo
Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A86 at 20 mg/kg reveal rapid oral absorption with a T max of 0.2-0.5 hr, C max of 1115 ng/mL, T 1/2 of 4.3 hr, and area under the curve (AUC) values of 2606 (ng*hr/mL) [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
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 12.5 mg/mL ( 36.29 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9033 mL | 14.5167 mL | 29.0335 mL |
| 5 mM | 0.5807 mL | 2.9033 mL | 5.8067 mL |
| 10 mM | 0.2903 mL | 1.4517 mL | 2.9033 mL |