ChemicalBook > CAS DataBase List > 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide

3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide

Product Name
3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide
CAS No.
860352-01-8
Chemical Name
3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide
Synonyms
CS-314;AZD 7762;White solid;AZD7762; AZD-7762;AZD-7762 Chk Inhibitor;AZD-7762, 10 mM in DMSO;1-(2-((S)-piperidin-3-ylcarbamoyl)-5-(3-fluorophenyl)thiophen-3-yl)urea;(S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide;5-(3-Fluorophenyl)-3-ureidothiophene-N-[(S)-piperidin-3-yl]-2-carboxamide;3-(carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide
CBNumber
CB72473926
Molecular Formula
C17H19FN4O2S
Formula Weight
362.42
MOL File
860352-01-8.mol
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3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide Property

Boiling point:
547.6±50.0 °C(Predicted)
Density 
1.38
storage temp. 
-20°
solubility 
Soluble in DMSO (up to at least 25 mg/ml).
pka
9.06±0.20(Predicted)
form 
solid
color 
Yellow or brown
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H302Harmful if swallowed

H318Causes serious eye damage

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P310Immediately call a POISON CENTER or doctor/physician.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
11491
Product name
AZD 7762
Purity
≥98%
Packaging
1mg
Price
$25
Updated
2024/03/01
Cayman Chemical
Product number
11491
Product name
AZD 7762
Purity
≥98%
Packaging
5mg
Price
$56
Updated
2024/03/01
Cayman Chemical
Product number
11491
Product name
AZD 7762
Purity
≥98%
Packaging
10mg
Price
$100
Updated
2024/03/01
Cayman Chemical
Product number
11491
Product name
AZD 7762
Purity
≥98%
Packaging
25mg
Price
$188
Updated
2024/03/01
TRC
Product number
A808125
Product name
AZD7762
Packaging
100mg
Price
$710
Updated
2021/12/16
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3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide Chemical Properties,Usage,Production

Description

Actively proliferating cells experience blocks at certain checkpoints in the cell cycle when DNA damage is detected. These checkpoints allow for DNA damage repair before further cell cycle progression. Targeting signaling pathways to selectively inhibit repair at these checkpoints in tumor cells is of considerable interest to cancer therapeutics. AZD 7762 selectively inhibits the activity of checkpoint kinases (Chk) 1 and Chk2 (IC50s = 5 nM) by competitively and reversibly binding their respective ATP-binding sites (Ki = 3.6 nM for Chk1). AZD 7762 abrogates DNA damage-induced S and G2 checkpoints with an EC50 value of 10 nM and potentiates the efficacy of DNA-damage repair prohibitive agents, gemcitabine and topotecan, both in vitro and in various tumor xenografts by modulating downstream checkpoint pathway proteins.

Uses

AZD 7762 is studied as an cancer therapeutic agent due to its selective inhibitory activities towards checkpoint kinases, chk1 and chk2 by reversibly binding their respective ATP-binding sites within tumor cells. Recent research has also indicated AZD 7762 to possess enhancing effects towards other chk1 inhibitor lethality in glioblastoma cells.

Definition

ChEBI: 3-(carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-3-piperidinyl]-2-thiophenecarboxamide is an aromatic amide and a member of thiophenes.

in vivo

In the rat H460-DNp53 xenograft study, AZD-7762 (AZD7762) potentiates the antitumor activity of NSC 613327 in a dose-dependent manner by a decrease in %T/C with increasing dose (48% and 32%, 10 and 20 mg/kg AZD-7762, respectively). In the mouse xenograft study in combination with CPT-11, SW620 established tumors are treated with vehicle, CPT-11 alone, AZD-7762 alone, or AZD-7762 in combination with CPT-11. AZD-7762 dosed alone shows insignificant antitumor activity, whereas CPT-11 alone displays striking and significant activity (%T/C with increasing dose is 9 and 1, respectively ). In combination with AZD-7762, %T/C increases significantly to -66% and -67%, respectively[1]. AZD7762 combination with CX-5461 induces cancer cell death of Tp53-null (Tp53-/-) Eμ-Myc lymphoma cells in vitro and in vivo[2].

IC 50

Chk1: 5 nM (IC50); Chk2: 5 nM (IC50)

References

[1] SONYA D ZABLUDOFF. AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies.[J]. Molecular Cancer Therapeutics, 2008, 7 9: 2955-2966. DOI:10.1158/1535-7163.mct-08-0492
[2] JAMES B MITCHELL. In vitro and in vivo radiation sensitization of human tumor cells by a novel checkpoint kinase inhibitor, AZD7762.[J]. Clinical Cancer Research, 2010, 16 7: 2076-2084. DOI:10.1158/1078-0432.ccr-09-3277
[3] MEREDITH A MORGAN. Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair.[J]. Cancer research, 2010, 70 12: 4972-4981. DOI:10.1158/0008-5472.can-09-3573
[4] HU LEI. Chk1 inhibitors overcome imatinib resistance in chronic myeloid leukemia cells[J]. Leukemia research, 2018, 64: Pages 17-23. DOI:10.1016/j.leukres.2017.11.007
[5] SYED AHMAD  John E S  Gary L Johnson. Identification of ponatinib and other known kinase inhibitors with potent MEKK2 inhibitory activity[J]. Biochemical and biophysical research communications, 2015, 463 4: Pages 888-893. DOI:10.1016/j.bbrc.2015.06.029
[6] YOUNG HWAN PARK . Repositioning of anti-cancer drug candidate, AZD7762, to an anti-allergic drug suppressing IgE-mediated mast cells and allergic responses via the inhibition of Lyn and Fyn[J]. Biochemical pharmacology, 2018, 154: Pages 270-277. DOI:10.1016/j.bcp.2018.05.012

3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide Preparation Products And Raw materials

Raw materials

Preparation Products

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3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide Suppliers

Canada 1 China 128 Germany 1 India 2 The Netherlands 1 United Kingdom 1 United States 19 Global 153
J & K SCIENTIFIC LTD.
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View Lastest Price from 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide manufacturers

Career Henan Chemical Co
Product
3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide 860352-01-8
Price
US $1.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
200kgs
Release date
2020-03-05
Career Henan Chemical Co
Product
3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide 860352-01-8
Price
US $1.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
200kgs
Release date
2020-03-05

860352-01-8, 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-ThiophenecarboxamideRelated Search:

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  • AZD7762; AZD-7762
  • CS-314
  • 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide
  • 5-(3-Fluorophenyl)-3-ureidothiophene-N-[(S)-piperidin-3-yl]-2-carboxamide
  • AZD 7762
  • White solid
  • 1-(2-((S)-piperidin-3-ylcarbamoyl)-5-(3-fluorophenyl)thiophen-3-yl)urea
  • 5-(3-Fluorophenyl)-3-ureidothiophene-N-[(S)-piperidin-3-yl]-2-carboxamide AZD 7762
  • AZD 7762 5-(3-Fluorophenyl)-3-ureidothiophene-N-[(S)-piperidin-3-yl]-2-carboxamide
  • (S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide
  • 2-Thiophenecarboxamide, 3-[(aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-
  • 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide USP/EP/BP
  • (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide hydrochloride
  • 3-(carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide
  • AZD-7762 Chk Inhibitor
  • AZD-7762, 10 mM in DMSO
  • 860352-01-8
  • 860325-01-8
  • api
  • Inhibitors