1. Cell Cycle/DNA Damage
  2. CDK

ON123300 

Cat. No.: HY-12624 Purity: 98.29%
Handling Instructions

ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, with little inhibitory activity against CDKs 1,2,5 and 8.

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

ON123300 Chemical Structure

ON123300 Chemical Structure

CAS No. : 1357470-29-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 158 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 792 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 1140 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, with little inhibitory activity against CDKs 1,2,5 and 8. IC50 value: 3.8 nM [1] Target: CDK4 in vitro: ON123300 is a novel kinase inhibitor, inhibits CDK4/6 and PI3K-δ and exhibits potent activity against mantle cell lymphomas (MCLs). [1] ON123300 is a low molecular weight multi-kinase inhibitor identified through a series of screens that supported further analyses for brain tumor chemotherapy. Biochemical assays indicated ON123300 was a strong inhibitor of Ark5 and CDK4 as well as growth factor receptor tyrosine kinases such as Beta-type platelet-derived growth factor receptor [PDGFRβ]. ON123300 inhibited U87 glioma cell proliferation with an IC50 = 3.4 ± 0.1 μM and reduced phosphorylation of Akt, yet it also unexpectedly induced Erk activation; both in a dose- and time-dependent manner that subsequently was attributed to relieving Akt-mediated C-Raf S259 inactivation and activating a p70S6K initiated PI3K negative feedback loop. [3]

IC50 & Target[1]

Cdk4/cyclin D1

3.87 nM (IC50)

CDK6/cyclinD1

9.82 nM (IC50)

ARK5

4.95 nM (IC50)

FGFR1

26 nM (IC50)

PDGFRβ

26 nM (IC50)

PI3K-δ

144 nM (IC50)

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3282 mL 11.6409 mL 23.2818 mL
5 mM 0.4656 mL 2.3282 mL 4.6564 mL
10 mM 0.2328 mL 1.1641 mL 2.3282 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

429.52

Formula

C₂₄H₂₇N₇O

CAS No.

1357470-29-1

SMILES

N#CC1=CC2=CN=C(NC3=CC=C(N4CCN(C)CC4)C=C3)N=C2N(C5CCCC5)C1=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
ON123300
Cat. No.:
HY-12624
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ON123300

Cat. No.: HY-12624