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Cdk4/6 Inhibitor IV

Product Name
Cdk4/6 Inhibitor IV
CAS No.
359886-84-3
Chemical Name
Cdk4/6 Inhibitor IV
Synonyms
GP-82996;Cdk4/6 Inhibitor IV;CGP-82996 (Synonyms: CINK4);Cyclohexanol, 4-[[6-(ethylamino)-2-[[1-(phenylmethyl)-1H-indol-5-yl]amino]-4-pyrimidinyl]amino]-,trans-
CBNumber
CB63136784
Molecular Formula
C27H32N6O
Formula Weight
456.58
MOL File
359886-84-3.mol
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Cdk4/6 Inhibitor IV Property

Boiling point:
755.4±70.0 °C(Predicted)
Density 
1.28±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
≤1mg/ml in ethanol;30mg/ml in DMSO;20mg/ml in dimethyl formamide
form 
crystalline solid
pka
15.05±0.40(Predicted)
color 
white to light brown
InChIKey
YVXCDLCJCIDFHE-AFARHQOCSA-N
SMILES
O[C@@H]1CC[C@@H](NC2=CC(NCC)=NC(NC3=CC=C(N(CC4=CC=CC=C4)C=C5)C5=C3)=N2)CC1
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Safety

WGK Germany 
WGK 3
Storage Class
11 - Combustible Solids
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1352
Product name
CINK4
Purity
≥95% (HPLC)
Packaging
25 mg
Price
$323
Updated
2025/07/31
Cayman Chemical
Product number
17974
Product name
Cdk4/6 Inhibitor IV
Purity
≥98%
Packaging
1mg
Price
$43
Updated
2024/03/01
Cayman Chemical
Product number
17974
Product name
Cdk4/6 Inhibitor IV
Purity
≥98%
Packaging
5mg
Price
$167
Updated
2024/03/01
Cayman Chemical
Product number
17974
Product name
Cdk4/6 Inhibitor IV
Purity
≥98%
Packaging
10mg
Price
$311
Updated
2024/03/01
TRC
Product number
C228135
Product name
Cdk4/6InhibitorIV
Packaging
10mg
Price
$275
Updated
2021/12/16
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Cdk4/6 Inhibitor IV Chemical Properties,Usage,Production

Uses

Cdk4/6 Inhibitor IV is a cell-permeable triaminopyrimidine compound and inhibitor of Cdk4/6.

Definition

ChEBI: 4-[[6-(ethylamino)-2-[[1-(phenylmethyl)-5-indolyl]amino]-4-pyrimidinyl]amino]-1-cyclohexanol is a member of indoles.

Biological Activity

cdk4/6 inhibitor iv is a cell-permeable triaminopyrimidine inhibitor for cdk4/cyclin d1 and cdk6/cyclin d1 [1].cyclin-dependent kinase 4 (cdk4) is an important cell cycle kinase, since its activity is required for initiating the phosphorylation of the retinoblastoma protein (prb). hyperphosphorylation of prb prevents cells from initiating dna synthesis, releases the sequestered transcription factors, leading to the loss of prb's growth-inhibitory function, thus allowing cells to enter s phase [1].

in vitro

cdk4/6 inhibitor iv showed an inhibitory effect on cdk4/cyclin d1 and cdk6/cyclin d1with the ic50 values of 1.5 and 5.6 μm, respectively. cdk4/6 inhibitor iv exihibited potent selectivity for cdk4/6 over cdk5/p35, c-met, v-abl, igf-1r, insulin receptor, cdk2/cyclin a, cdk2/cyclin e, cdk4/cyclin d2, cdk6/cyclin d2, and cdk1/cyclin b with the ic50 values ≥ 10-100 μm. in asynchronous cell lines, at 5-10 μm, cdk4/6 inhibitor iv blocked retinoblastoma protein phosphorylation at ser780 and ser795, inducing cell cycle arrest in the g1 phase and apoptosis.

in vivo

in mice xenografted with human hct116 colon carcinoma, treatment with of cdk4/6 inhibitor iv (i.p, 30 mg/kg) after 29 days suppressed tumor growth.

IC 50

Cdk4/cyclin D1: 1.5 μM (IC50); CDK6/cyclinD1: 5.6 μM (IC50); CDK5/p35: 25 μM (IC50); CDK2/cyclinA: >50 μM (IC50); CDK1/cyclinB: >100 μM (IC50); CDK2/cyclin E: >50 μM (IC50); CDK4/cyclin D2: >50 μM (IC50); Cdk6/cyclin D2: >50 μM (IC50); V-abl: >10 μM (IC50); c-met: >10 μM (IC50); IGF-1R: >10 μM (IC50); Insulin-R: >10 μM (IC50)

References

[1] soni r, o'reilly t, furet p, et al. selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4[j]. journal of the national cancer institute, 2001, 93(6): 436-446.

Cdk4/6 Inhibitor IV Preparation Products And Raw materials

Raw materials

Preparation Products

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Cdk4/6 Inhibitor IV Suppliers

Canada 1 China 23 India 1 Ukraine 1 United States 7 Global 33
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359886-84-3, Cdk4/6 Inhibitor IVRelated Search:


  • Cdk4/6 Inhibitor IV
  • Cyclohexanol, 4-[[6-(ethylamino)-2-[[1-(phenylmethyl)-1H-indol-5-yl]amino]-4-pyrimidinyl]amino]-,trans-
  • CGP-82996 (Synonyms: CINK4)
  • GP-82996
  • 359886-84-3
  • C27H32N6O