BS194

Product Name: BS194
CAS No.: 1092443-55-4
Chemical Name: BS194
Synonyms: BS194;CS-2655;BS-194;BS 194;BS194, 10 mM in DMSO;(2S,3S)-3-(7-(benzylaMino)-3-isopropylpyrazolo[1,5-a]pyriMidin-5-ylaMino)butane-1,2,4-triol;(2S,3S)-3-{[7-(benzylamino)-3-(propan-2-yl)pyrazolo[1,5-a]pyrimidin-5-yl]amino}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)-;BS-194,Antitumor,breast cancer,BS 194,xenografts,CDK,Inhibitor,MCF-7,colon cancer,retinoblastoma,BS194,anti-cancer,Cyclin dependent kinase,inhibit,HCT-116
CBNumber: CB42621131
Molecular Formula: C20H27N5O3
Formula Weight: 385.46
MOL File: 1092443-55-4.mol

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BS194 Property

Melting point:: 184-186 °C(Solv: acetonitrile (75-05-8))
Density: 1.33±0.1 g/cm3(Predicted)
pka: 13.54±0.20(Predicted)
form: Solid
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

American Custom Chemicals Corporation

Product number: INB0001452
Product name: BS-194
Purity: 95.00%
Packaging: 1MG
Price: $345.45
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: INB0001452
Product name: BS-194
Purity: 95.00%
Packaging: 5MG
Price: $497.2
Updated: 2021/12/16

DC Chemicals

Product number: DC8517
Product name: BS194
Purity: >98%
Packaging: 10mg
Price: $300
Updated: 2021/12/16

DC Chemicals

Product number: DC8517
Product name: BS194
Purity: >98%
Packaging: 50mg
Price: $1000
Updated: 2021/12/16

DC Chemicals

Product number: DC8517
Product name: BS194
Purity: >98%
Packaging: 100mg
Price: $1800
Updated: 2021/12/16

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BS194 Chemical Properties,Usage,Production

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).

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 (%)	C_max (min)	T_1/2 (min)
i.p.	10	73	30	147
p.o.	10	88	15	178
administration route	dose (mg/kg)	T_1/2 (min)	Cl (mL/min/kg)	V_z
i.v.	10	210	5	1391

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

BS194 Preparation Products And Raw materials

Raw materials

Preparation Products

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BS194 Suppliers

China 36 United Kingdom 1 United States 5 Global 42

SYN|thesis med chem P/L

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1092443-55-4, BS194Related Search:

CS-2655

BS-194;BS 194

BS194

(2S,3S)-3-(7-(benzylaMino)-3-isopropylpyrazolo[1,5-a]pyriMidin-5-ylaMino)butane-1,2,4-triol

1,2,4-Butanetriol, 3-[[3-(1-Methylethyl)-7-[(phenylMethyl)aMino]pyrazolo[1,5-a]pyriMidin-5-yl]aMino]-, (2S,3S)-

(2S,3S)-3-[[3-(1-Methylethyl)-7-[(phenylmethyl)amino]pyrazolo[1,5-a]pyrimidin-5-yl]amino]-1,2,4-butanetriol

BS-194,Antitumor,breast cancer,BS 194,xenografts,CDK,Inhibitor,MCF-7,colon cancer,retinoblastoma,BS194,anti-cancer,Cyclin dependent kinase,inhibit,HCT-116

(2S,3S)-3-{[7-(benzylamino)-3-(propan-2-yl)pyrazolo[1,5-a]pyrimidin-5-yl]amino}butane-1,2,4-triol

BS194, 10 mM in DMSO

1092443-55-4