Roniciclib

SKU: orb1307779

Description

Roniciclib (BAY 1000394) is a novel, orally bioavailable pan-cyclin-dependent kinase (CDK) inhibitor. It potently suppresses cell-cycle (CDK1/2/3/4) and transcriptional (CDK7/9) kinases with IC₅₀ values of 5-25 nM. This small molecule is utilized in cancer research to study cell cycle arrest and apoptosis in both in vitro and in vivo models.

Research Area

Cell Biology

Images & Validation

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Key Properties

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CAS Number	1223498-69-8
MW	430.44
Purity	98.84% (May vary between batches)
Formula	C₁₈H₂₁F₃N₄O₃S
SMILES	C[C@@H](O)[C@@H](C)Oc1nc(Nc2ccc(cc2)[S@](=N)(=O)C2CC2)ncc1C(F)(F)F
Target	CDK
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.62 mM);DMSO:249 mg/mL (578.48 mM)

Bioactivity

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Target IC50	CDK9-CyclinT1:5 nM\|CDK1-CyclinB:7 nM\|CDK4-CyclinD:11 nM\|CDK7-CyclinH-MAT1:25 nM\|CDK2-CyclinE:9 nM
In Vivo	Roniciclib has low blood clearance rates in mouse, rat, and dog (0.51, 0.78, and 0.50 Lh-1kg-1, respectively). Roniciclib strongly inhibits the growth of HeLa-MaTu tumors that have been grown to a size of approximately 50mm2 before the start of treatment. Roniciclib (1.5 and 1 mg/kg) treatment slow tumor growth to T/C values of 0.15 and 0.62, respectively. The addition of Roniciclib to cisplatin causes a strong tumor growth inhibition with T/C values of 0.01 (1.0 mg/kg Roniciclib) and -0.02 (1.5 mg/kg Roniciclib) . Read more...
In Vitro	Roniciclib inhibits the kinase activity of the cell-cycle CDKs CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclinD (IC50: 7, 9, and 11 nM, respectively). Roniciclibeffectively inhibits the proliferation of various human and murine tumor cell lines with a very balanced profile (mean IC50 on human tumor cells: 16 nM). The transcriptional CDKs CDK9/cyclin T1 and CDK7/cyclin H/MAT1 are inhibited in a similar range (5 and 25 nM) . Read more...

Storage & Handling

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Storage	store at low temperature,keep away from moisture \| 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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Cyclin dependent kinase, CDK7/Cyclin H/MAT1, CDK9/cyclin T1, CDK9/cyclinT1, CDK3/cyclinE, CDK4/cyclin D, CDK4/CyclinD, CDK2/cyclinE, CDK, CDK1/CyclinB, Cdk1/cyclin B, BAY 1000394, BAY1000394, BAY-1000394, inhibit, Inhibitor, Roniciclib

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Compound Identifiers

PubChem CID

71494949 ↗

Key Properties

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No computed properties available.

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Roniciclib (orb1307779)

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Roniciclib

Description

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Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

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Roniciclib (orb1307779)

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