2. Cell Cycle/DNA Damage
  3. CDK
  4. BS-194

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.

For research use only. We do not sell to patients.

BS-194 Chemical Structure

BS-194 Chemical Structure

CAS No. : 1092443-55-4

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1 mg USD 90 In-stock
5 mg USD 220 In-stock
10 mg USD 340 In-stock
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Based on 1 publication(s) in Google Scholar

BS-194 Related Antibodies

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Description

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].

IC50 & Target[1]

CDK2

3 nM (IC50)

CDK1

30 nM (IC50)

CDK5

30 nM (IC50)

CDK7

250 nM (IC50)

CDK9

90 nM (IC50)

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.

BS-194 Related Antibodies

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 (%) 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
Molecular Weight

385.46

Formula

C20H27N5O3
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5943 mL 12.9715 mL 25.9430 mL
5 mM 0.5189 mL 2.5943 mL 5.1886 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BS-1941092443-55-4BS194BS 194CDKCyclin dependent kinaseAntitumoranti-cancerMCF-7HCT-116retinoblastomaxenograftsbreast cancercolon cancerInhibitorinhibitorinhibit

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