1. Cell Cycle/DNA Damage
    Apoptosis
  2. TOPK
    CDK
    Apoptosis
  3. OTS964 hydrochloride

OTS964 hydrochloride 

Cat. No.: HY-12467 Purity: 99.05%
Handling Instructions

OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.

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

OTS964 hydrochloride Chemical Structure

OTS964 hydrochloride Chemical Structure

CAS No. : 1338545-07-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 189 In-stock
Estimated Time of Arrival: December 31
2 mg USD 110 In-stock
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5 mg USD 200 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
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25 mg USD 550 In-stock
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50 mg USD 850 In-stock
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100 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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  • Customer Review

Description

OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM[1]. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM[2].

IC50 & Target[1][2]

TOPK

28 nM (IC50)

CDK11B

40 nM (Kd)

In Vitro

OTS964 hydrochloride (10 nM; 48 hours) suppresses cancer cell proliferation[1].
OTS964 hydrochloride (10 nM; 48 hours) increases cancer cell death[1].
OTS964 (0.1-2 μM; 24 and 48 hours) increases the expression of LC3-II and decreases the expression of P62, both in a dose-dependent manner[3].

Cell Proliferation Assay[1]

Cell Line: LU-99 cells
Concentration: 10 nM
Incubation Time: 48 hours
Result: Suppressed cancer cell proliferation.

Apoptosis Analysis[1]

Cell Line: LU-99 cells
Concentration: 10 nM
Incubation Time: 48 hours
Result: Increased cancer cell death.

Western Blot Analysis[3]

Cell Line: Hs683 cells, H4 cells
Concentration: 0.1, 1, 2 μM
Incubation Time: 24 and 48 hours
Result: Increased the expression of LC3-II and decreased the expression of P62, both in a dose-dependent manner.
In Vivo

OTS964 hydrochloride (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression[1].
OTS964 hydrochloride (oral administration; 50 or 100 mg/kg/day for 2 weeks) ultimately achieves complete tumor regression[1].

Animal Model: Nude mice bearing LU-99 lung cancer cells[1]
Dosage: 40 mg/kg
Administration: Intravenously; on days 1, 4, 8, 11, 15, and 18
Result: The tumors continued shrinking even after the treatment and finally revealed complete regression.
Animal Model: Nude mice bearing LU-99 lung cancer cells[1]
Dosage: 50 or 100 mg/kg
Administration: Oral administration; once every day for 2 weeks
Result: Achieved complete tumor regression.
Molecular Weight

428.97

Formula

C₂₃H₂₅ClN₂O₂S

CAS No.

1338545-07-5

SMILES

OC1=CC(C)=C2C(C3=C(SC=C3)C(N2)=O)=C1C4=CC=C([[email protected]@H](C)CN(C)C)C=C4.Cl

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 : ≥ 83.33 mg/mL (194.26 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3312 mL 11.6558 mL 23.3117 mL
5 mM 0.4662 mL 2.3312 mL 4.6623 mL
10 mM 0.2331 mL 1.1656 mL 2.3312 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.05%

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Product Name:
OTS964 hydrochloride
Cat. No.:
HY-12467
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