Casein Kinase inhibitor A51
- Product Name
- Casein Kinase inhibitor A51
- CAS No.
- 2079068-74-7
- Chemical Name
- Casein Kinase inhibitor A51
- Synonyms
- T9175;BTX-A51;CKIα inhibitor A51;CKIα inhibitor A51;Casein Kinase inhibitor A51;BTX-A51 (Casein Kinase inhibitor A51);trans-N1-(5-Chloro-4-(5-(cyclopropylmethyl)-1-methyl-1H-pyrazol-4-yl)pyrimidin-2-yl)cyclohexane-1,4-diamine;1,4-Cyclohexanediamine, N1-[5-chloro-4-[5-(cyclopropylmethyl)-1-methyl-1H-pyrazol-4-yl]-2-pyrimidinyl]-, trans-
- CBNumber
- CB14667710
- Molecular Formula
- C18H25ClN6
- Formula Weight
- 360.88
- MOL File
- 2079068-74-7.mol
Casein Kinase inhibitor A51 Property
- Boiling point:
- 570.0±60.0 °C(Predicted)
- Density
- 1.48±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- pka
- 10.41±0.70(Predicted)
- form
- Solid
- color
- Off-white to brown
N-Bromosuccinimide Price
- Product number
- DC11250
- Product name
- CaseinKinaseinhibitorA51
- Purity
- >98%
- Packaging
- 5mg
- Price
- $550
- Updated
- 2021/12/16
Casein Kinase inhibitor A51 Chemical Properties,Usage,Production
Uses
BTX-A51 (Casein Kinase inhibitor A51) is a potent and orally active casein kinase 1α (CK1α) inhibitor. BTX-A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities[1].
Biological Activity
Casein Kinase inhibitor A51 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities[1]. Similar to CKIα depletion, Casein Kinase inhibitor A51 (0.05-3.2 μM; 18 hours) treatment of RKO cells abolished most of the Ser45 phosphorylation signal and the consecutive GSK3 phosphorylation cascade resulting in stabilization of β-catenin[1]. Casein Kinase inhibitor A51 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 A51 (0.08-2 μM; 6.5 hours) abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. Casein Kinase inhibitor A51 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]. Oral treatment is initiated at 8 days (Casein Kinase inhibitor A51; 5 mg/kg/day) after leukemia cell inoculation, at which the percentage of leukemia cells in the BM is more than 1.5% of all cells. all A51-treated mice have normal organ morphology and histology and normal blood counts[1].Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A51 at 20 mg/kg reveal rapid oral absorption with a Tmax of 0.5-2 hr, Cmax of 1060 ng/mL, T1/2 of 2.5 hr, and area under the curve (AUC) values of 3680 (ng*hr/mL)[1].
in vivo
Oral treatment is initiated at 8 days (BTX-A51; 5 mg/kg/day) after leukemia cell inoculation, at which the percentage of leukemia cells in the BM is more than 1.5% of all cells. all A51-treated mice have normal organ morphology and histology and normal blood counts[1].
Pharmacokinetic studies of the inhibitor BTX-A51 at 20 mg/kg reveal rapid oral absorption with a Tmax of 0.5-2 hr, Cmax of 1060 ng/mL, T1/2 of 2.5 hr, and area under the curve (AUC) values of 3680 (ng*hr/mL)[1].
IC 50
CKIα; CDK7: 1.3 nM (Kd); CDK9: 4 nM (Kd)
References
[1]. Waleed Minzel, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018 Sep 20;175(1):171-185.e25.
Casein Kinase inhibitor A51 Preparation Products And Raw materials
Raw materials
Preparation Products
Casein Kinase inhibitor A51 Suppliers
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- United States
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- United States
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View Lastest Price from Casein Kinase inhibitor A51 manufacturers
- Product
- T9175;A51 2079068-74-7
- Price
- US $0.00-0.00/MG
- Min. Order
- 1MG
- Purity
- 99% HPLC
- Supply Ability
- 10000
- Release date
- 2024-09-20