Company Name: |
Fan De(Beijing) Biotechnology Co., Ltd.
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Tel: |
15911056312 |
Email: |
liming@bio-fount.com |
Products Intro: |
Product Name:(2S,3R)-3-(3,4-DIFLUOROPHENYL)-2-(4-FLUOROPHENYL)-4-HYDROXY-N-((3S)-2-OXO-5-PHENYL-2,3-1H-BENZO[E][1,4]DIAZEPIN-3-YL)BUTYRAMIDE CAS:2081093-21-0 Purity:97.0% Package:5mg
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Company Name: |
TargetMol Chemicals Inc.
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Tel: |
4008200310 |
Email: |
marketing@tsbiochem.com |
Products Intro: |
Product Name:CHMFL-ABL/KIT-155;CHMFL ABL/KIT 155,CHMFLABL/KIT155 CAS:2081093-21-0 Purity:98% Package:5 mg
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| (2S,3R)-3-(3,4-DIFLUOROPHENYL)-2-(4-FLUOROPHENYL)-4-HYDROXY-N-((3S)-2-OXO-5-PHENYL-2,3-1H-BENZO[E][1,4]DIAZEPIN-3-YL)BUTYRAMIDE Basic information |
Product Name: | (2S,3R)-3-(3,4-DIFLUOROPHENYL)-2-(4-FLUOROPHENYL)-4-HYDROXY-N-((3S)-2-OXO-5-PHENYL-2,3-1H-BENZO[E][1,4]DIAZEPIN-3-YL)BUTYRAMIDE | Synonyms: | (2S,3R)-3-(3,4-DIFLUOROPHENYL)-2-(4-FLUOROPHENYL)-4-HYDROXY-N-((3S)-2-OXO-5-PHENYL-2,3-1H-BENZO[E][1,4]DIAZEPIN-3-YL)BUTYRAMIDE;(2S,3R)-3-(3,4-DIFLUOROPHENYL)-2-(4-FLUOROPHENYL)-4-HYDROXY-N-((3S)-2-OXO-5-PHENYL-2,3-DIHYDRO-1H-BENZO[E][1,4]DIAZEPIN-3-YL)-BUTYRAMIDE;COMPOUND 34;GAMMA-SECRETASE INHIBITOR XIX;CHMFL-ABL/KIT-155;CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155;CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; COMPOUND 34);Benzamide, N-[4-methyl-3-[[1-[(6-methyl-3-pyridinyl)carbonyl]-4-piperidinyl]oxy]phenyl]-4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)- | CAS: | 2081093-21-0 | MF: | C33H38F3N5O3 | MW: | 609.68 | EINECS: | | Product Categories: | | Mol File: | Mol File | |
| (2S,3R)-3-(3,4-DIFLUOROPHENYL)-2-(4-FLUOROPHENYL)-4-HYDROXY-N-((3S)-2-OXO-5-PHENYL-2,3-1H-BENZO[E][1,4]DIAZEPIN-3-YL)BUTYRAMIDE Chemical Properties |
Boiling point | 660.5±55.0 °C(Predicted) | density | 1.271±0.06 g/cm3(Predicted) | storage temp. | Store at -20°C | solubility | Soluble in DMSO | pka | 12.67±0.70(Predicted) |
| (2S,3R)-3-(3,4-DIFLUOROPHENYL)-2-(4-FLUOROPHENYL)-4-HYDROXY-N-((3S)-2-OXO-5-PHENYL-2,3-1H-BENZO[E][1,4]DIAZEPIN-3-YL)BUTYRAMIDE Usage And Synthesis |
Description | CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis[1].
IC50: 46 nM (type II ABL), 75 nM (c-KIT), 81 nM (BLK), 227 nM (CSF1R), 116 nM (DDR1), 325 nM (DDR2), 12 nM (LCK), 80 nM (PDGFRβ)[1] CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) exhibits anti-proliferation activities in the BCR-ABL dependent CML cancer cell lines such as K562 (GI50: 0.027 µM), MEG-01 (GI50: 0.02 µM), and KU812 (GI50: 0.056 µM). It also potently inhibits the growth of c-KIT dependent GISTs cancer cell lines including GIST-T1 (GI50: 0.023 µM), GIST-882 (GI50: 0.095 µM) but not c-KIT independent GIST-48B (GI50: 3.96 µM) [1]. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) (25-100 mg/kg; p.o.; once daily for 28 days) shows dose-dependent tumor progression suppression without apparent toxicity in female nu/nu mice bearing established K562 tumor xenografts[1]. | References | [1]. Wang Q, et al. Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. J Med Chem. 2017 Jan 12;60(1):273-289. |
| (2S,3R)-3-(3,4-DIFLUOROPHENYL)-2-(4-FLUOROPHENYL)-4-HYDROXY-N-((3S)-2-OXO-5-PHENYL-2,3-1H-BENZO[E][1,4]DIAZEPIN-3-YL)BUTYRAMIDE Preparation Products And Raw materials |
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