1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. Ilginatinib hydrochloride

Ilginatinib hydrochloride (Synonyms: NS-018 hydrochloride)

Cat. No.: HY-19631B Purity: 98.02%
Handling Instructions

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).

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

Ilginatinib hydrochloride Chemical Structure

Ilginatinib hydrochloride Chemical Structure

CAS No. : 1239358-85-0

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 267 In-stock
Estimated Time of Arrival: December 31
5 mg USD 285 In-stock
Estimated Time of Arrival: December 31
10 mg USD 395 In-stock
Estimated Time of Arrival: December 31
25 mg USD 580 In-stock
Estimated Time of Arrival: December 31
50 mg USD 870 In-stock
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100 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
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Description

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).

IC50 & Target[1]

JAK2

0.72 nM (IC50)

Tyk2

22 nM (IC50)

JAK1

33 nM (IC50)

JAK3

39 nM (IC50)

In Vitro

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). Ilginatinib hydrochloride also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. Ilginatinib hydrochloride shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene (expressing a constitutively activated JAK2) with IC50 of 11-120 nM, but has only minimal cytotoxicity against most other hematopoietic cell lines that have no constitutively activated JAK2[1].
Ilginatinib hydrochloride (0.5 μM) preferentially suppresses colony-forming unitgranulocyte/macrophage (CFU-GM) formation from myelodysplastic syndrome (MDS)-derived bone marrow mononuclear cells (BMMNCs). Ilginatinib hydrochloride (1 μM) suppresses the phosphorylation of STAT3 (the downstream kinase of JAK2) in CFU-GM-forming cells from MDS patients[2].

In Vivo

Ilginatinib hydrochloride (NS-018 hydrochloride) (12.5, 25, 50, 100 mg/kg, p.o.) potently prolongs the survival of mice and reduces splenomegaly in a mouse Ba/F3-JAK2V617F disease model[1].
Ilginatinib hydrochloride (25, 50 mg/kg, p.o.) significantly reduces leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improves nutritional status, and prolongs survival in JAK2V617F transgenic mice[1].

Clinical Trial
Molecular Weight

425.89

Formula

C₂₁H₂₁ClFN₇

CAS No.

1239358-85-0

SMILES

[H]Cl.CN1N=CC(C2=CC(N[[email protected]](C3=CC=C(F)C=C3)C)=NC(NC4=NC=CN=C4)=C2)=C1

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 : ≥ 35 mg/mL (82.18 mM)

H2O : 2 mg/mL (4.70 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3480 mL 11.7401 mL 23.4802 mL
5 mM 0.4696 mL 2.3480 mL 4.6960 mL
10 mM 0.2348 mL 1.1740 mL 2.3480 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

Bone marrow mononuclear cells (BMMNCs) from healthy volunteers and myelodysplastic syndrome (MDS) patients are incubated in MethoCult GF H4434 methylcellulose medium containing various hematopoietic cytokines at 1.0 × 105 cells/mL with or without Ilginatinib (NS-018) at 37°C in a humidified atmosphere of 5% CO2. Commercially available purified normal human CD34-positive (CD34+) BM cells are used as a control. Burst-forming unit-erythroid (BFU-E) and colonyforming unit-granulocyte/macrophage (CFU-GM) colonies are counted under an inverted microscope on day 14 of culture[2].

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

Animal Administration
[1]

Mice[1]
Female BALB/c nude mice are placed in blanket cages in an environment maintained at 21-25°C and 45-65% relative humidity, with artificial illumination for 12 h and a ventilation frequency of at least 15 times/h. They are allowed free access to food pellets and tap water. Ba/F3-JAK2V617F cells (106 per mouse) are inoculated intravenously into 7-week-old mice. Administration of vehicle (0.5% methylcellulose) or Ilginatinib (NS-018) twice daily by oral gavage begins the day after cell inoculation. Survival is monitored daily, and moribund mice are humanely killed and their time of death is recorded for purposes of survival analysis. In a parallel study, all mice are humanely killed after 8 days of administration, and their spleens are removed and weighed[1].

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

References
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Keywords:

IlginatinibNS-018NS018NS 018JAKJanus kinaseorallybioavailableJAK2JAK1JAK3Tyk2Inhibitorinhibitorinhibit

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Product Name:
Ilginatinib hydrochloride
Cat. No.:
HY-19631B
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