2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. RGB-286147

RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with IC50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity.

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RGB-286147 Chemical Structure

RGB-286147 Chemical Structure

CAS No. : 784211-09-2

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Based on 1 publication(s) in Google Scholar

RGB-286147 Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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Description

RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with IC50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity[1].

IC50 & Target[1]

CDK1/cyclinB

48 nM (IC50)

CDK2/E

15 nM (IC50)

CDK4/D1

839 nM (IC50)

cdk6/cyclin D3

232 nM (IC50)

In Vitro

RGB-286147 (50-100 nM; 24-48 hr) induces cell cycle arrest in the G1 phase, causes a marked inhibition of DNA replication, and induces apoptosis in HCT116 cells[1].
RGB-286147 (100 nM; 48 hr) results in proteolytic cleavage of PARP in HCT116 cells[1].
RGB-286147 (24-72 hr) shows potent and irreversible cell killing activity in HCT116 cells. The IC50 value for inhibition of colony formation by RGB-286147 is 57 nM[1].
RGB-286147 (48 hr) exhibits broad anti-tumor activity with an average GI50 value of <10 nM for 60 tumorigenic cell lines. And also inhibits growth of non-cycling HCT116 cells with an IC50 value of 40 nM[1].

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

RGB-286147 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 50 nM and 100 nM
Incubation Time: 24 or 48 hr
Result: Caused a marked inhibition of DNA replication and induced cell cycle arrest.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 100 nM
Incubation Time: 48 hr
Result: Resulted in proteolytic cleavage of PARP.
Molecular Weight

473.35

Formula

C23H22Cl2N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(N(C3=C(Cl)C=CC=C3Cl)N=C2C(C)C)N=C(CC4=CC=C(OCCO)C=C4)N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (63.38 mM; Need ultrasonic and warming; 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 2.1126 mL 10.5630 mL 21.1260 mL
5 mM 0.4225 mL 2.1126 mL 4.2252 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 (sealed storage, away from moisture). 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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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥98.0%

COA (250 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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 2.1126 mL 10.5630 mL 21.1260 mL 52.8150 mL
5 mM 0.4225 mL 2.1126 mL 4.2252 mL 10.5630 mL
10 mM 0.2113 mL 1.0563 mL 2.1126 mL 5.2815 mL
15 mM 0.1408 mL 0.7042 mL 1.4084 mL 3.5210 mL
20 mM 0.1056 mL 0.5282 mL 1.0563 mL 2.6408 mL
25 mM 0.0845 mL 0.4225 mL 0.8450 mL 2.1126 mL
30 mM 0.0704 mL 0.3521 mL 0.7042 mL 1.7605 mL
40 mM 0.0528 mL 0.2641 mL 0.5282 mL 1.3204 mL
50 mM 0.0423 mL 0.2113 mL 0.4225 mL 1.0563 mL
60 mM 0.0352 mL 0.1761 mL 0.3521 mL 0.8803 mL
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RGB-286147 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:

RGB-286147784211-09-2RGB286147RGB 286147CDKApoptosisCyclin dependent kinaseCDK1CDK2CDK-related kinasesCRKcell apoptosisanti-tumor activityATP-competitivecell cycle arrestInhibitorinhibitorinhibit

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