Company Name: |
ShangHai Caerulum Pharma Discovery Co., Ltd.
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Tel: |
18149758185 18149758185 |
Email: |
sales-cpd@caerulumpharma.com |
Products Intro: |
Product Name:(2S,3S,4S)-N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-(6-methyl-4-(trifluoromethyl)pyridin-2-yl)-5-oxopyrrolidine-2-carboxamide CAS:2607138-82-7 Package:10g;1g;100mg
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Company Name: |
ATK CHEMICAL COMPANY LIMITED
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Tel: |
021-51619050 13301662590 |
Email: |
mandy@atkchemical.com |
Products Intro: |
CAS:2607138-82-7 Purity:98% HPLC Package:5MG;10MG;50MG;100MG,1G,5G
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| 2-Pyrrolidinecarboxamide, N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-[6-methyl-4-(trifluoromethyl)-2-pyridinyl]-5-oxo-, (2S,3S,4S)- Basic information |
Product Name: | 2-Pyrrolidinecarboxamide, N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-[6-methyl-4-(trifluoromethyl)-2-pyridinyl]-5-oxo-, (2S,3S,4S)- | Synonyms: | 2-Pyrrolidinecarboxamide, N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-[6-methyl-4-(trifluoromethyl)-2-pyridinyl]-5-oxo-, (2S,3S,4S)-;(2S,3S,4S)-N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-(6-methyl-4-(trifluoromethyl)pyridin-2-yl)-5-oxopyrrolidine-2-carboxamide;ART812;ART812, 10 mM in DMSO | CAS: | 2607138-82-7 | MF: | C19H16ClF4N3O4 | MW: | 461.79 | EINECS: | | Product Categories: | | Mol File: | 2607138-82-7.mol | ![2-Pyrrolidinecarboxamide, N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-[6-methyl-4-(trifluoromethyl)-2-pyridinyl]-5-oxo-, (2S,3S,4S)- Structure](CAS/20210305/GIF/2607138-82-7.gif) |
| 2-Pyrrolidinecarboxamide, N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-[6-methyl-4-(trifluoromethyl)-2-pyridinyl]-5-oxo-, (2S,3S,4S)- Chemical Properties |
Boiling point | 691.2±55.0 °C(Predicted) | density | 1.588±0.06 g/cm3(Predicted) | storage temp. | Store at -20°C | pka | 11.99±0.60(Predicted) | form | Solid | color | White to off-white |
| 2-Pyrrolidinecarboxamide, N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-[6-methyl-4-(trifluoromethyl)-2-pyridinyl]-5-oxo-, (2S,3S,4S)- Usage And Synthesis |
Biological Activity | ART812 is an orally active DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. ART812 has an IC50 value of 240 nM for cell based microhomology-mediated end joining (MMEJ)[1][2].
ART812 (0-40 μM) elicits Polθ inhibitor sensitivity in MDA-MB-436 SHLD2 knockout cells[1].
ART812 (100 mg/kg; p.o. daily for 76 days) shows significant tumour inhibition in rats bearing established MDA-MB-436 BRCA1/SHLD2 defective tumours (volume 250-350 mm3)[1]. | References | [1]. Zatreanu D, et al. Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance. Nat Commun. 2021 Jun 17;12(1):3636. [2]. Peter BLENCOWE, et al. Preparation of heterocyclic compounds for use in the treatment of cancer. WO2021028643 A1. |
| 2-Pyrrolidinecarboxamide, N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-[6-methyl-4-(trifluoromethyl)-2-pyridinyl]-5-oxo-, (2S,3S,4S)- Preparation Products And Raw materials |
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