| Identification | Back Directory | [Name]
BS194 | [CAS]
1092443-55-4 | [Synonyms]
BS194
CS-2655
BS-194;BS 194
(2S,3S)-3-(7-(benzylaMino)-3-isopropylpyrazolo[1,5-a]pyriMidin-5-ylaMino)butane-1,2,4-triol
(2S,3S)-3-[[3-(1-Methylethyl)-7-[(phenylmethyl)amino]pyrazolo[1,5-a]pyrimidin-5-yl]amino]-1,2,4-butanetriol
1,2,4-Butanetriol, 3-[[3-(1-Methylethyl)-7-[(phenylMethyl)aMino]pyrazolo[1,5-a]pyriMidin-5-yl]aMino]-, (2S,3S)- | [Molecular Formula]
C20H27N5O3 | [MOL File]
1092443-55-4.mol | [Molecular Weight]
385.46 |
| Chemical Properties | Back Directory | [Melting point ]
184-186 °C(Solv: acetonitrile (75-05-8)) | [density ]
1.33±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
13.54±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
BS-194 is as a potent, orally available inhibitor of cyclin-dependent protein kinases (CDKs) 1, 2, 7 and 9 | [Uses]
BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer[1]. | [in vivo]
BS-194 (compound 4K, intraperitoneal injection, 5 or 10 mg/kg, twice daily for 14 days) inhibits tumor growth with no apparent toxicity in MCF-7 tumor xenografts[1].
BS-194 (i.p., i.v., p.o., 10 mg/kg) is orally bioavailable, with elimination half-lives of 147 min (i.p.), 210 min (i.v.), and 178 min (p.o.) respectively[1].
BS-194 (oral gavage, 25 mg/mL) reduces rapid RB and PolII (RNA polymerase II) phosphorylation, but recovery within 24 h in nu/nu-BALB/c athymic nude mice[1].
BS-194 (oral gavage, 25 mg/kg, daily for 14 days) inhibits tumor growth in HCT116 tumor xenografts, with no significant loss in animal weights[1]. | Animal Model: | Nude mice bearing MCF-7 cell[1] | | Dosage: | 5 or 10 mg/kg, twice daily for 14 days. | | Administration: | Intraperitoneal injection | | Result: | Inhibited tumor growth in a dose-dependent manner (30% and 40% reduction at 5 and 10 mg/kg dose, respectively). |
| Animal Model: | HCT116 tumor xenografts[1] | | Dosage: | 25 mg/kg, daily for 14 days. | | Administration: | Oral gavage | | Result: | Inhibited tumor growth by 50% reduction at 25 mg/kg.
Decreased levels of Rb phosphorylation at Ser807/811 and Thr821 (in resected tumors).
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| Animal Model: | Mice (pharmacokinetic assay)[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection, intravenous injection, oral administration | | Result: | Pharmacokinetic profile of BS-194 (compound 4k).
| administration route | dose (mg/kg) | bioavail-ability (%) | Cmax (min) | T1/2 (min) | | i.p. | 10 | 73 | 30 | 147 | | p.o. | 10 | 88 | 15 | 178 | | administration route | dose (mg/kg) | T1/2 (min) | Cl (mL/min/kg) | Vz | | i.v. | 10 | 210 | 5 | 1391 |
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| [IC 50]
CDK2: 3 nM (IC50); CDK1: 30 nM (IC50); CDK5: 30 nM (IC50); CDK7: 250 nM (IC50); CDK9: 90 nM (IC50) | [References]
[1] Dean A Heathcote, et al. A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J Med Chem. 2010 Dec 23;53(24): DOI:10.1021/jm100732t |
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Lynnchem
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86-(0)29-85992781 17792393971 |
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Novachemistry
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Twochem Co.Ltd.
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cn.twochem.com |
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Cckinase, Inc.
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+1 (732)236-3202 |
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www.cckinase.com |
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