GP-82996

SKU: orb1704985

Description

GP-82996 (CINK4) is a selective CDK4/6 inhibitor with IC50 values of 1.5 μM (CDK4/cyclin D1) and 5.6 μM (CDK6/cyclin D1). It induces apoptosis in U2OS osteosarcoma cells in vitro and serves as a valuable research tool for studying cell cycle dysregulation in cancer models.

Research Area

Cell Biology

Images & Validation

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Key Properties

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CAS Number	359886-84-3
MW	456.58
Purity	99.94%
Formula	C₂₇H₃₂N₆O
SMILES	C(N1C=2C(=CC(NC=3N=C(N[C@@H]4CC[C@@H](O)CC4)C=C(NCC)N3)=CC2)C=C1)C5=CC=CC=C5
Target	CDK
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.38 mM);DMSO:50 mg/mL (109.51 mM)

Bioactivity

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Target IC50	CDK2-CyclinE:>50 μM\|IGF-1R:>10 μM\|CDK2-CyclinA:>50 μM\|Insulin Receptor:>10 μM\|CDK1-cyclinB:>100 μM\|CDK4-CyclinD2:>50 μM\|CDK6-CyclinD2:>50 μM\|c-Met:>10 μM\|Cdk4-CyclinD1:1.5 μM\|CDK5-p35:25 μM\|CDK6-CyclinD1:5.6 μM\|V-abl:>10 μM Read more...
In Vivo	GP-82996 (30 mg/kg, i.p. for 29 days) significantly reduced final tumor volume compared to the vehicle control in mouse xenograft models . In female BALB/c nu/nu mice (19-21 g) with HCT116 tumors (100 mm^3), the compound was administered intraperitoneally at 30 mg/kg every 12 hours for 29 days, leading to smaller tumor volumes than the control group . Read more...
In Vitro	GP-82996, at concentrations of 5 and 10 μM applied for 24 hours, causes a G1 phase arrest and an increase in the G0-G1/S ratio in U2OS (p16 negative) and MRC-5 (p16 positive) cells, while reducing the hyperphosphorylation of pRb without affecting CDK4 levels in these cell lines. In U2OS cells, a 48-hour exposure to 10μM of GP-82996 results in apoptosis in 83% of the population. Additionally, GP-82996 inhibits the proliferation of A549, H358, SKLU-1, H23, and PC14 cells, with IC50 values around 4-7 μM after 72 hours of treatment. The compound also induces G1 arrest in A549 and H23 cells at concentrations of 3, 5, and 10 μM over 48 hours and enhances the sensitivity of KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23) to Paclitaxel with varied concentrations (1, 3, 5, 10 μM) over 72 hours. A combination of GP-82996 (10 μM) and Paclitaxel (3 nM) over 72 hours notably increases apoptosis in A549 and H23 cells. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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CDK4/CyclinD1, Cdk4/6 Inhibitor IV, CDK6/cycD1, CINK 4, CINK4, CINK-4, GP 82996, GP82996, GP-82996

Quality Guarantee

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Compound Identifiers

PubChem CID

24825971 ↗

Key Properties

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No computed properties available.

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GP-82996

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

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GP-82996 (orb1704985)

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