Ilginatinib maleate

SKU: orb1309315

Description

Ilginatinib maleate

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	1354799-87-3
MW	505.5
Purity	99.74%
Formula	C₂₅H₂₄FN₇O₄
SMILES	OC(=O)\C=C/C(O)=O.C[C@H](Nc1cc(cc(Nc2cnccn2)n1)-c1cnn(C)c1)c1ccc(F)cc1
Target	Tyrosine Kinases,JAK
Solubility	DMSO:50 mg/mL (98.91 mM);H2O:< 0.1 mg/mL (insoluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.96 mM)

Bioactivity

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Target IC50	JAK1:33 nM\|JAK2:0.72 nM\|TYK2:22 nM\|JAK3:39 nM
In Vivo	Ilginatinib maleate(NS-018 maleate) preferentially suppressed in vitro erythropoietin-independent endogenous colony formation from polycythemia vera patients. NS-018 also markedly reduced splenomegaly and prolonged the survival of mice inoculated with Ba/F3 cells harboring JAK2V617F. In addition, NS-018 significantly reduced leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improved nutritional status, and prolonged survival in JAK2V617F transgenic mice. suggest that NS-018 will be a promising candidate for the treatment of MPNs. Read more...
In Vitro	Ilginatinib maleate(NS-018 maleate) is highly active against JAK2 with a 50% inhibition (IC(50)) of <1 n, and had 30-50-fold greater selectivity for JAK2 over other JAK-family kinases, such as JAK1, JAK3 and tyrosine kinase 2. In addition to JAK2, NS-018 inhibited Src-family kinases. NS-018 showed potent antiproliferative activity against cell lines expressing a constitutively activated JAK2 (the JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene; IC(50)=11-120 n), but showed only minimal cytotoxicity against most other hematopoietic cell lines without a constitutively activated JAK2. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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TyrosineKinases, Tyrosine Kinases, Tyk2, Inhibitor, NS018, NS-018, NS018 Maleate, NS-018 Maleate, NS-018 maleate, NS 018, NS 018 Maleate, JAK2, JAK1, JAK, Janus kinase, inhibit, JAK3, Ilginatinib, Ilginatinib maleate, Ilginatinib Maleate, orally, bioavailable

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Compound Identifiers

PubChem CID

56599590 ↗

Key Properties

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No computed properties available.

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