2. JAK/STAT Signaling
  3. Pim
  4. CX-6258 hydrochloride hydrate

CX-6258 hydrochloride hydrate 

Cat. No.: HY-18095A Purity: 98.61%
COA Handling Instructions

CX-6258 hydrochloride hydrate is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.

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

CX-6258 hydrochloride hydrate Chemical Structure

CX-6258 hydrochloride hydrate Chemical Structure

CAS No. : 1353858-99-7

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Solution
10 mM * 1 mL in DMSO USD 164 In-stock
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10 mg USD 192 In-stock
50 mg USD 540 In-stock
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Description

CX-6258 hydrochloride hydrate is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively[1].

IC50 & Target

IC50: 5 nM (Pim-1), 25 nM (Pim-2), 16 nM (Pim-3)[1]
In Vitro

CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively[1].
CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells[2].
CX-6258 treatment results in a significant reduction in NKX3.1 half-life[2].

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

Western Blot Analysis[1]

Cell Line: MV-4-11 human AML cells.
Concentration: 0.1 μM, 1 μM, 10 μM.
Incubation Time: 2 hours.
Result: Caused dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.
In Vivo

CX-6258 (50-100 mg/kg; p.o; daily; over a period of 21 days) exhibits robust in vivo efficacy in two Pim kinases driven tumor models[1].

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

Animal Model: Nude mice, MV-4-11 xenograft models[1]
Dosage: 50 mg/kg, 100 mg/kg.
Administration: Oral administration; once daily; over a period of 21 days.
Result: Exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI.
Molecular Weight

516.42

Appearance

Solid

Formula

C26H27Cl2N3O4
CAS No.
SMILES

O=C1NC2=CC=C(Cl)C=C2/C1=C\C3=CC=C(C4=CC=CC(C(N5CCCN(C)CC5)=O)=C4)O3.[H]Cl.O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (48.41 mM; Need ultrasonic)

H2O : 7.14 mg/mL (13.83 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9364 mL 9.6820 mL 19.3641 mL
5 mM 0.3873 mL 1.9364 mL 3.8728 mL
10 mM 0.1936 mL 0.9682 mL 1.9364 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  20% HP-β-CD in saline

    Solubility: 20 mg/mL (38.73 mM); Suspended solution; Need ultrasonic and warming and heat to 48°C

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

CX-6258 hydrochloride1353858-99-7PimPim kinasesBad4E-BP1Inhibitorinhibitorinhibit

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