CRT0066101

ChemicalBook > CAS DataBase List > CRT0066101

Product Name: CRT0066101
CAS No.: 1883545-60-5
Chemical Name: CRT0066101
Synonyms: CS-2578;CRT0066101 hcl;CRT0066101 2HCL;CRT0066101 (CRT-0066101;CRT0066101 dihydrochloride;2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride;Inhibitor,CRT-0066101 dihydrochloride,CRT0066101,CRT0066101 dihydrochloride,Protein kinase D,CRT-0066101,CRT 0066101,PKD,inhibit
CBNumber: CB63164875
Molecular Formula: C18H23ClN6O
Formula Weight: 374.87
MOL File: 1883545-60-5.mol

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CRT0066101 Property

storage temp.: Store at -20°C
solubility: insoluble in H2O; ≥15.65 mg/mL in DMSO; ≥4.49 mg/mL in EtOH with ultrasonic
form: solid
color: Off-white to light yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC

Product number: C782018
Product name: CRT0066101
Packaging: 5mg
Price: $280
Updated: 2021/12/16

ApexBio Technology

Product number: A8679
Product name: CRT0066101
Packaging: 10mg
Price: $150
Updated: 2021/12/16

ApexBio Technology

Product number: A8679
Product name: CRT0066101
Packaging: 10mM(in 1mL DMSO)
Price: $180
Updated: 2021/12/16

ApexBio Technology

Product number: A8679
Product name: CRT0066101
Packaging: 100mg
Price: $1800
Updated: 2021/12/16

DC Chemicals

Product number: DC20928
Product name: CRT0066101
Purity: >98%
Packaging: 1g
Price: $2500
Updated: 2021/12/16

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CRT0066101 Chemical Properties,Usage,Production

Biological Activity

crt 0066101 is a specific inhibitor of all pkd isoforms. increasingly studies reveals that pkd family members play an important role in regulating several cellular processes and activities, including chromatin organization, golgi function, gene expression, cell survival, adhesion, motility, differentiation, dna synthesis and proliferation. by suppressing pkd, crt 0066101 is supposed to ameliorate symptoms of pancreatic cancer. [1]

in vitro

in panc-1 cell line based assays, crt0066101 was reported to reduce bromodeoxyuridine incorporation; increase cell apoptosis; suppress neurotensin-induced pkd1/2 activation; block neurotensin-induced hsp27 phosphorylation; interrupt pkd1-mediated nf-κb activation as well as down-regulate expression of nf-κb-dependent proliferative and pro-survival proteins. [1]

in vivo

in panc-1 subcutaneous xenograft model, orally administration of crt0066101 at the dosage of 80 mg/kg/d for 24 days significantly suppressed pancreatic cancer growth. moreover, when crt0066101 reached its peak concentration (12 μmol/l) in tumor model, the expression of activated pkd1/2 in the treated tumor explants was substantially decreased. it was concluded that crt0066101 given orally at 80 mg/kg/d for 21 days in panc-1 orthotropic model suppressed tumor growth potently in vivo. [1]

target

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> PKD2
(Cell-free assay)

Target	Value
PKD1 (Cell-free assay)	1 nM
PKD3 (Cell-free assay)	2 nM
2.5 nM

IC 50

a potent protein kinase d (pkd) antagonist with the ic50 of 1, 2.5 and 2 nm for pkd1, pkd2, pkd3 respectively.

storage

Store at -20°C

References

[1]harikumar kb, kunnumakkara1 ab, ochi n, tong z, deorukhkar a, sung b, kelland l, jamieson s, sutherland r, raynham t, charles m, bagherzadeh a, foxton c, boakes a, farooq m, maru d, diagaradjane p, matsuo y, smith j, gelovani j, krishnan s, aggarwal bb, rozengurt e, ireson cr, and guha s. a novel small-molecule inhibitor of protein kinase d blocks pancreatic cancer growth in vitro and in vivo. mol cancer ther. 2010 may. 9(5): 113646.

CRT0066101 Preparation Products And Raw materials

Raw materials

Preparation Products

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CRT0066101 Suppliers

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1883545-60-5, CRT0066101Related Search:

CRT0066101 2HCL

CRT0066101 dihydrochloride

2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride

CRT0066101 (CRT-0066101

CS-2578

CRT0066101 hcl

Inhibitor,CRT-0066101 dihydrochloride,CRT0066101,CRT0066101 dihydrochloride,Protein kinase D,CRT-0066101,CRT 0066101,PKD,inhibit

1883545-60-5

C18H22N6O2HCl