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CRT-0066101

Product Name
CRT-0066101
CAS No.
956123-34-5
Chemical Name
CRT-0066101
Synonyms
CRT0066101;CRT 0066101;CRT-0066101;SCJXQZZYGYLKJG-CQSZACIVSA-N;Phenol, 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)-;6-6-(2R)-2-Aminobutylamino-1H-pyrimidin-2-ylidene-4-(1-methylpyrazol-4-yl)cyclohexa-2,4-dien-1-one,hydrochloride
CBNumber
CB42667706
Molecular Formula
C18H22N6O
Formula Weight
338.41
MOL File
956123-34-5.mol
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CRT-0066101 Property

Boiling point:
518.5±50.0 °C(Predicted)
Density 
1.30±0.1 g/cm3(Predicted)
storage temp. 
-20°C
form 
powder
pka
8.10±0.50(Predicted)
color 
white to beige
Water Solubility 
H2O: 15mg/mL, clear
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1507
Product name
CRT0066101 hydrochloride
Purity
≥98% (HPLC)
Packaging
5MG
Price
$111
Updated
2025/07/31
Sigma-Aldrich
Product number
SML1507
Product name
CRT0066101 hydrochloride
Purity
≥98% (HPLC)
Packaging
25MG
Price
$447
Updated
2025/07/31
Tocris
Product number
4975
Product name
CRT0066101
Purity
≥98%(HPLC)
Packaging
10
Price
$291
Updated
2021/12/16
Usbiological
Product number
255050
Product name
CRT 0066101
Packaging
10mg
Price
$545
Updated
2021/12/16
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CRT-0066101 Chemical Properties,Usage,Production

Uses

CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively[1]. CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7?nM. CRT0066101 exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects[1][2][3].

Biochem/physiol Actions

CRT0066101 is a very potent inhibitor of Protein Kinase D (PKD) isoforms with IC50 values for PKD-1, -2 and -3 = 1, 2.5 and 2 nM, respecitively. CRT0066101 has been shown to have anticancer activity. CRT0066101 potently inhibits proliferation of PANC-1 pancreatic cells, and blocks migration and invasion of U87MG glioblastoma cells. CRT0066101 has also been shown to decrease growth of primary tumors and metastasis of ER(-) breast cancers.

in vivo

CRT0066101 (80 mg/kg/day; oral gavage; once daily; for 21 days) in Panc-1 orthotopic model potently blocks tumor growth in vivo[1].
CRT0066101 (10 mg/kg, i.p., every two days for 3 times) exhibits a protective effect against LPS-induced pneumonia and alleviates lung damage in C57BL/6J mice[3].

Animal Model:CR-UK nu/nu mice injected with Panc-1 cells[1]
Dosage:80 mg/kg/day
Administration:Oral gavage; once daily; for 21 days
Result:Potently blocked tumor growth in vivo.
Animal Model:LPS (HY-D1056)-induced lung injury in C57BL/6J mice[3]
Dosage:10 mg/kg
Administration:i.p., once every two days for 3 times
Result:Inhibited the expression of MyD88 and TLR4, inhibited the phosphorylation of NF-κB, ERK and JNK.

IC 50

PKD1: 1 nM (IC50); PKD2: 2.5 nM (IC50); PKD3: 2 nM (IC50); PIM2: 135.7 nM (IC50)

References

[1] Harikumar KB, et al. 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):1136-46. DOI:10.1158/1535-7163.MCT-09-1145
[2] Xi Chen, et al. Identification and assessment of new PIM2 inhibitors for treating hematologic cancers: A combined approach of energy-based virtual screening and machine learning evaluation. Arch Pharm (Weinheim). 2024 Jan 23:e2300516. DOI:10.1002/ardp.202300516
[3] Cui B, et al., Small molecule inhibitor CRT0066101 inhibits cytokine storm syndrome in a mouse model of lung injury. Int Immunopharmacol. 2023 Jul;120:110240. DOI:10.1016/j.intimp.2023.110240

CRT-0066101 Preparation Products And Raw materials

Raw materials

Preparation Products

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CRT-0066101 Suppliers

China 30 United States 2 Global 32
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
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51395
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SPIRO PHARMA
Tel
Fax
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Email
eric_feng1954@126.com
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China
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EMMX Biotechnology LLC
Tel
888-539-0666
Fax
888-539-0666
Email
info@emmx.com
Country
United States
ProdList
8447
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Chengdu Novel Biomedical Co., Ltd.
Tel
028-85255396 18302801538
Fax
028-85255396
Email
cdnovell@163.com
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China
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2389
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Suzhou Chenrui Biotechnology Co. LTD
Tel
17625585511
Fax
qq：1580084073
Email
1580084073@qq.com
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China
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959
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Nantong Hi-Future Biotechnology Co., Ltd
Tel
18051384581
Email
sales@chemhifuture.com
Country
China
ProdList
2995
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Suzhou Zhixin Biotechnology Co., Ltd.
Tel
0512-65118909 18100677375
Email
sales@szzxbio.com
Country
China
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2993
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ShenZhen Trendseen Biological Technology Co.,Ltd.
Tel
13417589054;
Email
trendseenbio@gmail.com
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China
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Suzhou Haiben Pharmaceutical Co., Ltd
Tel
19353112242
Email
1816280386@qq.com
Country
China
ProdList
8045
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Baoji Didu Pharmaceutical and Chemical Co., Ltd
Tel
029-81145305 17791533577
Email
1021@dideu.com
Country
China
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10009
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956123-34-5, CRT-0066101Related Search:


  • CRT 0066101
  • CRT0066101
  • CRT-0066101
  • SCJXQZZYGYLKJG-CQSZACIVSA-N
  • 6-6-(2R)-2-Aminobutylamino-1H-pyrimidin-2-ylidene-4-(1-methylpyrazol-4-yl)cyclohexa-2,4-dien-1-one,hydrochloride
  • Phenol, 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)-
  • 956123-34-5