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Cas Database

802536-13-6

802536-13-6

Identification

Synonyms:N,1-dimethyl-8-[(1-methylsulfonylpiperidin-4-yl)amino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamide;N,1-dimethyl-8-((1-(methylsulfonyl)piperidin-4-yl)amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;1H-Pyrazolo[4,3-h]quinazoline-3-carboxaMide, 4,5-dihydro-N,1-diMethyl-8-[[1-(Methylsulfonyl)-4-piperidinyl]aMino]-

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Safety information and MSDS view more

  • Signal Word:no data available

  • Hazard Statement:no data available

  • First-aid measures: General adviceConsult a physician. Show this safety data sheet to the doctor in attendance.If inhaled If breathed in, move person into fresh air. If not breathing, give artificial respiration. Consult a physician. In case of skin contact Wash off with soap and plenty of water. Consult a physician. In case of eye contact Rinse thoroughly with plenty of water for at least 15 minutes and consult a physician. If swallowed Never give anything by mouth to an unconscious person. Rinse mouth with water. Consult a physician.

  • Fire-fighting measures: Suitable extinguishing media Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide. Wear self-contained breathing apparatus for firefighting if necessary.

  • Accidental release measures: Use personal protective equipment. Avoid dust formation. Avoid breathing vapours, mist or gas. Ensure adequate ventilation. Evacuate personnel to safe areas. Avoid breathing dust. For personal protection see section 8. Prevent further leakage or spillage if safe to do so. Do not let product enter drains. Discharge into the environment must be avoided. Pick up and arrange disposal. Sweep up and shovel. Keep in suitable, closed containers for disposal.

  • Handling and storage: Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Avoid exposure - obtain special instructions before use.Provide appropriate exhaust ventilation at places where dust is formed. For precautions see section 2.2. Store in cool place. Keep container tightly closed in a dry and well-ventilated place.

  • Exposure controls/personal protection:Occupational Exposure limit valuesBiological limit values Handle in accordance with good industrial hygiene and safety practice. Wash hands before breaks and at the end of workday. Eye/face protection Safety glasses with side-shields conforming to EN166. Use equipment for eye protection tested and approved under appropriate government standards such as NIOSH (US) or EN 166(EU). Skin protection Wear impervious clothing. The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace. Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique(without touching glove's outer surface) to avoid skin contact with this product. Dispose of contaminated gloves after use in accordance with applicable laws and good laboratory practices. Wash and dry hands. The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and the standard EN 374 derived from it. Respiratory protection Wear dust mask when handling large quantities. Thermal hazards

Supplier and reference price view more

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  • Manufacture/Brand:American Custom Chemicals Corporation
  • Product Description:4,5-DIHYDRO-N,1-DIMETHYL-8-[[1-(METHYLSULFONYL)-4-PIPERIDINYL]AMINO]-1H-PYRAZOLO-[4,3-H]QUINAZOLINE-3-CARBOXAMIDE 95.00%
  • Packaging:5MG
  • Price:$ 499.88
  • Delivery:In stock
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Relevant articles and documentsAll total 2 Articles be found

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitor

Traquandi, Gabriella,Ciomei, Marina,Ballinari, Dario,Casale, Elena,Colombo, Nicoletta,Croci, Valter,Fiorentini, Francesco,Isacchi, Antonella,Longo, Antonio,Mercurio, Ciro,Panzeri, Achille,Pastori, Wilma,Pevarello, Paolo,Volpi, Daniele,Roussel, Patrick,Vulpetti, Anna,Brasca, Maria Gabriella

experimental part, p. 2171 - 2187 (2010/08/19)

Abnormal proliferation mediated by disruption of the mechanisms that keep the cell cycle under control is a hallmark of virtually all cancer cells. Compounds targeting complexes between cyclin-dependent kinases (CDKs) and cyclins (Cy) and inhibiting their activity are regarded as promising antitumor agents to complement the existing therapies. An expansion of pyrazolo[4,3-h]quinazoline chemical class oriented to the development of three points of variability was undertaken leading to a series of compounds able to inhibit CDKs both in vitro and in vivo. Starting from the CDK selective but poorly soluble hit compound 1, we succeeded in obtaining several compounds showing enhanced inhibitory activity both on CDKs and on tumor cells and displaying improved physical properties and pharmacokinetic behavior. Our study led to the identification of compound 59 as a highly potent, orally bioavailable CDK inhibitor that exhibited significant in vivo efficacy on the A2780 ovarian carcinoma xenograft model. The demonstrated mechanisms of action of compound 59 on cancer cell lines and its ability to inhibit tumor growth in vivo render this compound very interesting as potential antineoplastic agent.

Process route upstream and downstream products

Process route

8-amino-N,1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide

8-amino-N,1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide

1-(methylsulfonyl)piperidin-4-one
218780-53-1

1-(methylsulfonyl)piperidin-4-one

N,1-dimethyl-8-([1-(methylsulfonyl)piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
802536-13-6

N,1-dimethyl-8-([1-(methylsulfonyl)piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide

Conditions
Conditions Yield
With sodium tris(acetoxy)borohydride; trifluoroacetic acid; In N,N-dimethyl-formamide; for 18h;
72%
N,1-dimethyl-8-([1-(methylsulfonyl)piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
802536-13-6

N,1-dimethyl-8-([1-(methylsulfonyl)piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide

Conditions
Conditions Yield

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