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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
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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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

DC Chemicals
Product number
DC11250
Product name
CaseinKinaseinhibitorA51
Purity
>98%
Packaging
5mg
Price
$550
Updated
2021/12/16
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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

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Casein Kinase inhibitor A51 Suppliers

China 24 United States 3 Global 27
ShangHai Caerulum Pharma Discovery Co., Ltd.
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18149758185
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sales-cpd@caerulumpharma.com
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China
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Shanghai Beckham Medical Technology Co., Ltd
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13816613772
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QQ: 12922499
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huahero21@sina.com
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Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
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021-65675885
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info@efebio.com
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China
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Wellman Pharmaceutical Group Limited
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027-027-83778875 15807197853
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027-83991220
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15807197853@163.com
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Henan Alpha Chemical Co., Ltd.
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0371-55055611 18137792234
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3002694073@qq.com
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China
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Zhengzhou Alfa Chemical Co.,Ltd
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+8618530059196
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sale04@alfachem.cn
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China
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DC Chemicals
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021-58447131 13564518121
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doncunbiosci@gmail.com
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China
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Changzhou Chenhong Biotechnology Co., Ltd.
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+86-0519-85788828 +86-13775037613
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sales@chemrenpharm.com
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China
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Wuxi Donghe Pharmaceutical Technology Co., Ltd.
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63313187 15358055255
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63313187@qq.com
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Guangzhou Younan Technology Co., Ltd
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020-82000279 18988941452
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YN_research@163.com
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Chunchuang (Wuhan) Technology Co., Ltd
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15727060112
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yutianchun2007@126.com
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China
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Bide Pharmatech Ltd.
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400-1647117 13681763483
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product02@bidepharm.com
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China
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TargetMol Chemicals Inc.
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4008200310
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marketing@tsbiochem.com
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China
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Hangzhou Runyan Medical Technology Co., LTD
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571-13989459766 18112526015
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sales@runyanpharma.com
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China
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Nantong QuanYi Biotechnology Co., Ltd
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0513-66337626 18051384581
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sales@chemhifuture.com
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Nanjing Shizhou Biology Technology Co.,Ltd
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025-85560043 15850508050
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Nantong Hanfang Biotechnology Co. , Ltd.
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hanfangpharma@126.com; 18616537568
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hanfangpharma@126.com
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China
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Anhui JYHX CO., LTD.
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Chengdu Peter-like Biotechnology Co., Ltd.
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Sangon Biotech (Shanghai) Co.,Ltd.
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China
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Aikon International Limited
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025-58851090 13408877820
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2850281427@qq.com
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China
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10000
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HangZhou RunYan Pharma Technology Co.,LTD.
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+8618882027439
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sales2@runyanpharma.com
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302
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Biorbyt Ltd.
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Jinan Fanxun Biological Technology Co., LTD
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qingyan7590@163.com
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View Lastest Price from Casein Kinase inhibitor A51 manufacturers

HangZhou RunYan Pharma Technology Co.,LTD.
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

2079068-74-7, Casein Kinase inhibitor A51Related Search:


  • Casein Kinase inhibitor A51
  • CKIα inhibitor A51
  • BTX-A51
  • 1,4-Cyclohexanediamine, N1-[5-chloro-4-[5-(cyclopropylmethyl)-1-methyl-1H-pyrazol-4-yl]-2-pyrimidinyl]-, trans-
  • T9175
  • 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
  • CKIα inhibitor A51
  • 2079068-74-7