Cat. No.: HY-14372

BS-194

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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.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.13%
CAS No.: 1092443-55-4
Formule: C₂₀H₂₇N₅O₃
Masse moléculaire:385.46

Stockage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

BS-194 Chemical Structure

CAS No.: 1092443-55-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

CDK2

3 nM (IC₅₀)

CDK1

30 nM (IC₅₀)

CDK5

30 nM (IC₅₀)

CDK7

250 nM (IC₅₀)

CDK9

90 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform CDK :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	0.2 μM Compound: 4k, BS-194	Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay	[PMID: 21080703]
COLO 205	GI₅₀	0.12 μM Compound: 4k, BS-194	Antiproliferative activity against human COLO205 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human COLO205 cells after 72 hrs by sulforhodamine B assay	[PMID: 21080703]
HCT-116	GI₅₀	0.1 μM Compound: 4k, BS-194	Antiproliferative activity against human HCT116 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human HCT116 cells after 72 hrs by sulforhodamine B assay	[PMID: 21080703]
HepG2	GI₅₀	1 μM Compound: 4k, BS-194	Antiproliferative activity against human HepG2 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human HepG2 cells after 72 hrs by sulforhodamine B assay	[PMID: 21080703]
HepG2	IC₅₀	1 μM Compound: IV; 4k, BS-194	Cytotoxicity against human HepG2 cells Cytotoxicity against human HepG2 cells	[PMID: 33784602]
HUVEC	GI₅₀	6.3 μM Compound: 4k, BS-194	Antiproliferative activity against human HUVEC cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human HUVEC cells after 72 hrs by sulforhodamine B assay	[PMID: 21080703]
MCF-10A	GI₅₀	0.1 μM Compound: 4k, BS-194	Antiproliferative activity against human MCF10A cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human MCF10A cells after 72 hrs by sulforhodamine B assay	[PMID: 21080703]
MCF7	GI₅₀	0.3 μM Compound: 4k, BS-194	Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay	[PMID: 21080703]
MCF7	IC₅₀	0.3 μM Compound: IV; 4k, BS-194	Cytotoxicity against human MCF7 cells Cytotoxicity against human MCF7 cells	[PMID: 33784602]
MDA-MB-231	GI₅₀	0.3 μM Compound: 4k, BS-194	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay	[PMID: 21080703]
PC-3	GI₅₀	0.5 μM Compound: 4k, BS-194	Antiproliferative activity against human PC3 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human PC3 cells after 72 hrs by sulforhodamine B assay	[PMID: 21080703]
SAOS-2	GI₅₀	0.25 μM Compound: 4k, BS-194	Antiproliferative activity against human Saos2 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human Saos2 cells after 72 hrs by sulforhodamine B assay	[PMID: 21080703]
SK-OV-3	GI₅₀	0.3 μM Compound: 4k, BS-194	Antiproliferative activity against human SKOV3 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human SKOV3 cells after 72 hrs by sulforhodamine B assay	[PMID: 21080703]

In Vitro

BS-194 (compound 4k, 72 h) inhibits various cancer cells (MCF-7, MDA-MB-231, MCF-10A, CPLO-205, HCT-116, A549, SaOS2, PC3 ,HepG2, SK-Ov-3) growth, with IC₅₀ values ranging from 100 nM to 1 μM^[1].
BS-194 (10 μM, 24 h) promotes cell cycle arrest in in S and G2/M phases in HCT116 cells^[1].
BS-194 (10 μM, 24 h) inhibits phosphorylation of CDK substrates, and promotes cyclin loss in HCT116 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:

HCT116
Concentration:

0, 0.01, 0.1, 1, 10 μM
Incubation Time:

24 h
Result:

Showed a significant reduction in G1, and increased in S and G2/M phases.

Western Blot Analysis^[1]

Cell Line:

HCT116
Concentration:

0, 0.1, 10, 20 μM
Incubation Time:

0, 0.1, 10, 20 μM
Result:

Inhibited the phosphorylation of the CDK2 substrate RB (retinoblastoma) at Ser-780, Ser-795, Ser-801, Ser-807/Ser-811, and Thr-821.
Inhibited levels of cyclin A, cyclin B, and cyclin D1.
Inhibited phosphorylation of Thr-170 of CDK2.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

Chemical Information

CAS No. 1092443-55-4
Appearance Solid
Masse moléculaire 385.46
Formule C₂₀H₂₇N₅O₃
Color White to off-white
SMILES

OC[C@@H](O)[C@@H](NC1=NC2=C(C(C)C)C=NN2C(NCC3=CC=CC=C3)=C1)CO
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (259.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5943 mL

12.9715 mL

25.9430 mL

5 mM

0.5189 mL

2.5943 mL

5.1886 mL

10 mM

0.2594 mL

1.2972 mL

2.5943 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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): [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5943 mL	12.9715 mL	25.9430 mL	64.8576 mL
	5 mM	0.5189 mL	2.5943 mL	5.1886 mL	12.9715 mL
	10 mM	0.2594 mL	1.2972 mL	2.5943 mL	6.4858 mL
	15 mM	0.1730 mL	0.8648 mL	1.7295 mL	4.3238 mL
	20 mM	0.1297 mL	0.6486 mL	1.2972 mL	3.2429 mL
	25 mM	0.1038 mL	0.5189 mL	1.0377 mL	2.5943 mL
	30 mM	0.0865 mL	0.4324 mL	0.8648 mL	2.1619 mL
	40 mM	0.0649 mL	0.3243 mL	0.6486 mL	1.6214 mL
	50 mM	0.0519 mL	0.2594 mL	0.5189 mL	1.2972 mL
	60 mM	0.0432 mL	0.2162 mL	0.4324 mL	1.0810 mL
	80 mM	0.0324 mL	0.1621 mL	0.3243 mL	0.8107 mL
	100 mM	0.0259 mL	0.1297 mL	0.2594 mL	0.6486 mL

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BS-194

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Voir tous les produits spécifiques à Isoform CDK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

BS-194

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Voir tous les produits spécifiques à Isoform CDK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

BS-194 Related Classifications

HY-14372 Related Classifications