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D-I03

Product Name
D-I03
CAS No.
688342-78-1
Chemical Name
D-I03
Synonyms
D-I03;D-I03 (D103);D-I03, 10 mM in DMSO;1-(2-(Diethylamino)ethyl)-3-(2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl)thiourea;Thiourea, N-[2-(diethylamino)ethyl]-N'-[2-(4-ethyl-1-piperazinyl)-4-methyl-6-quinolinyl]-
CBNumber
CB44844707
Molecular Formula
C23H36N6S
Formula Weight
428.64
MOL File
688342-78-1.mol
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D-I03 Property

Boiling point:
582.0±60.0 °C(Predicted)
Density 
1.147±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO: ≥ 100 mg/mL (233.30 mM)
form 
Solid
pka
12.00±0.70(Predicted)
color 
Off-white to light yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2496
Product name
D-I03
Purity
≥98% (HPLC)
Packaging
5mg
Price
$40.8
Updated
2024/03/01
Sigma-Aldrich
Product number
SML2496
Product name
D-I03
Purity
≥98% (HPLC)
Packaging
25mg
Price
$411
Updated
2024/03/01
ChemScene
Product number
CS-0087335
Product name
D-I03
Purity
99.73%
Packaging
5mg
Price
$80
Updated
2021/12/16
ChemScene
Product number
CS-0087335
Product name
D-I03
Purity
99.73%
Packaging
10mg
Price
$145
Updated
2021/12/16
ChemScene
Product number
CS-0087335
Product name
D-I03
Purity
99.73%
Packaging
25mg
Price
$330
Updated
2021/12/16
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D-I03 Chemical Properties,Usage,Production

Biological Activity

D-I03 is a selective inhibitor of RAD52 with a corresponding Kd value of 25.8 μM. D-I03 inhibits ssDNA annealing via RAD52 and D-loop formation with IC50 values of 5 μM and 8 μM, respectively.

in vitro

D-I03 (0-10 μM; on days 1 and 3; Capan-1 and UWB1.289 cells) treatment preferentially suppressed the growth of Capan-1 and UWB1.289 cells in a concentration-dependent manner .
D-I03 inhibits RAD52 foci formation induced by cisplatin in BCR-ABL1-positive BRCA1-deficient 32Dcl3 murine hematopoietic cell line that expresses GFP-RAD52. In the presence of D-I03 (2.5 μM), the fraction of cells with RAD52 foci is decreased, from 38.7% to 171%; at the same time, the fraction of Cisplatin-treated cells without foci is increased from 48.4% to 71.9%. D-I03 does not effect on RAD51 foci induced by Cisplatin. Also, D-I03 alone induce neither RAD51 foci nor RAD52 foci (in BRCA1-deficient cells) indicating low genotoxicity of D-I03.

Cell Proliferation Assay

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Cell Line: Capan-1 (BRCA2 ? ) and UWB1 .289 (BRCA1 + ) cells
Concentration: 0 μM, 2.5 μM, 5 μM, or 10 μM
Incubation Time: On days 1 and 3
Result: Preferentially suppressed the growth of Capan-1 and UWB1.289 cells.

in vivo

D-I03 (50 mg/kg/day; intraperitoneal injection; daily; for 7 days; nu/nu mice) treatment reduces BRCA1-deficient MDA-MB-436 tumor growth . Talazoparib puls D-I03 does not affect the growth of BRCA1-proficient tumors and does not exert any significant toxicity against normal tissues and organs.
Pharmacokinetic and toxicity studies indicate that maximal tolerated dose of D-I03 is ≥50 mg /kg, and t 1/2 is 23.4 hours, resulting in >1 μM maximal concentration in peripheral blood.

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Animal Model: Nu/nu mice injected with BRCA1-deficient MDA-MB-436 cells
Dosage: 50 mg/kg/day
Administration: Intraperitoneal injection; daily; for 7 days
Result: Reduced BRCA1-deficient MDA-MB-436 tumor growth.

target

TargetValue
RAD52
(Cell-free assay)		 25.8 μM(Ki)

D-I03 Preparation Products And Raw materials

Raw materials

Preparation Products

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D-I03 Suppliers

China 22 United States 4 Global 26
Shanghai Beckham Medical Technology Co., Ltd
Tel
021-13816613772 13816613772
Fax
QQ: 12922499
Email
huahero21@sina.com
Country
China
ProdList
724
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55
ShangHai Biochempartner Co.,Ltd
Tel
17754423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8011
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62
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
32161
Advantage
58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
Email
sales@chemegen.com
Country
China
ProdList
11218
Advantage
58
Wuhan Topule
Tel
+86-02787215551 +86-19945035818
Fax
027-87215551
Email
2936752263@qq.com
Country
China
ProdList
8084
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58
Shanghai Sunway Pharmaceutical Technology Co.,Ltd.
Tel
021-51816796-820 13611835272
Fax
021-5161 3951
Email
sales2@sunwaypharm.com
Country
China
ProdList
44457
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58
Hubei Kele Fine Chemical Co., Ltd
Tel
027-59101668 19945030958
Fax
027-59101668
Email
2881924765@qq.com
Country
China
ProdList
7920
Advantage
58
Bide Pharmatech Ltd.
Tel
400-1647117 13681763483
Email
product02@bidepharm.com
Country
China
ProdList
62075
Advantage
58
InvivoChem
Tel
13549236410
Email
sales@invivochem.cn
Country
China
ProdList
6753
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58
Wuhan Yingnuo Pharmaceutical Technology Co., Ltd.
Tel
+86-027-59232304 15387063101
Email
2881924050@qq.com
Country
China
ProdList
9997
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58

688342-78-1, D-I03Related Search:


  • D-I03 (D103)
  • D-I03
  • Thiourea, N-[2-(diethylamino)ethyl]-N'-[2-(4-ethyl-1-piperazinyl)-4-methyl-6-quinolinyl]-
  • 1-(2-(Diethylamino)ethyl)-3-(2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl)thiourea
  • D-I03, 10 mM in DMSO
  • 688342-78-1