1. Cell Cycle/DNA Damage
    PI3K/Akt/mTOR
    Epigenetics
  2. CDK
    AMPK
  3. ON123300

ON123300 

Cat. No.: HY-12624 Purity: 98.52%
Handling Instructions

ON123300, a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent ON123300 causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors. ON123300 inhibits CDK6 with an IC50 of 9.82 nM.

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

ON123300 Chemical Structure

ON123300 Chemical Structure

CAS No. : 1357470-29-1

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10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
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10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 792 In-stock
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100 mg USD 1140 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

ON123300, a strong and brain-penetrant[1] multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent ON123300 causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors[2]. ON123300 inhibits CDK6 with an IC50 of 9.82 nM[3].

IC50 & Target[2][3]

Cdk4/cyclin D1

3.9 nM (IC50)

ARK5

5 nM (IC50)

CDK6/cyclinD1

9.82 nM (IC50)

RET

9.2 nM (IC50)

FYN

11 nM (IC50)

FGFR1

26 nM (IC50)

PDGFRβ

26 nM (IC50)

PI3K-δ

144 nM (IC50)

In Vitro

ON123300 inhibits U87 glioma cell proliferation with an IC50 of 3.4±0.1 μM[2]. ON123300 (1 and 10 μM) inhibits cell proliferation in a panel of 11 glioma models including a patient-derived model (GBM10)[2].
ON123300 (6.3 μM; 1 h) reduces phosphorylation of Akt and its downstream signaling components, P70S6K, 40S rpS6 and Rb S780, yet ON123300 induces Erk activation in U87 cells; both in a dose- and time-dependent manner[2]. ON123300 inhibits PI3Kδ with the IC50 of 144nM[3].

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

Cell Cytotoxicity Assay[2]

Cell Line: U87 glioma cells
Concentration: 0, 4, 8, 12, 16 μM
Incubation Time: 72 hour
Result: Had an IC50 equal to 3.4±0.1 μM.

Western Blot Analysis[2]

Cell Line: U87 cells
Concentration: 6.3 μM
Incubation Time: 1 h
Result: Inhibited phosphorylation of Akt (at S473 site) and its downstream signaling components, P70S6K, 40S ribosomal protein S6 (rpS6) and Rb S780 (decreased to 40.1%; 31.8 %; 60.5%; 54.5% relatively to control), yet increased p-Erk (increased to 120% relative to control).
In Vivo

ON123300 decreases p-Akt expression and increases p-Erk activity in brain tumors upon administration at both IV doses of 5 mg/kg and 25 mg/kg in U87 brain tumor-bearing mouse. The half-life (T1/2) is 1.5 h for 5 mg/kg and 25 mg/kg in plasma[2].

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

Animal Model: NIH Swiss nude mice bearing U87 glioma model[2].
Dosage: 5 mg/kg or 25 mg/kg
Administration: IV bolus at a dose of either 5 mg/kg or 25 mg/kg via a tail vein.
Result: The p-Akt rapidly declined and reached nadir values of 73% and 60% of control within 30 min after 5 mg/kg and 25 mg/kg dose levels, respectively.
Clinical Trial
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (38.81 mM; ultrasonic and warming and heat to 60°C)

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
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Keywords:

ON123300ON 123300ON-123300CDKAMPKCyclin dependent kinaseAMP-activated protein kinaseRTKkinasebrainpenetrationmultiCDK4CDK6Ark5PDGFRβFGFR1RETFYNtumorU87gliomaInhibitorinhibitorinhibit

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ON123300
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