Ilginatinib hydrochloride

SKU: orb1309314

Description

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	1239358-85-0
MW	425.89
Purity	99.55%
Formula	C₂₁H₂₁ClFN₇
SMILES	Cl.C[C@H](Nc1cc(cc(Nc2cnccn2)n1)-c1cnn(C)c1)c1ccc(F)cc1
Target	Tyrosine Kinases,JAK
Solubility	DMSO:60 mg/mL (140.88 mM);10% DMSO+90% Saline:2.5 mg/mL (5.87 mM);H2O:2 mg/mL (4.7 mM)

Bioactivity

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Target IC50	TYK2:22 nM\|JAK3:39 nM\|JAK1:33 nM\|JAK2:0.72 nM
In Vivo	Ilginatinib hydrochloride(NS-018 hydrochloride) preferentially suppressed in vitro erythropoietin-independent endogenous colony formation from polycythemia vera patients.NS-018 also markedly reduced splenomegaly and prolonge 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 andidate fo the treatment of MPN. Read more...
In Vitro	Ilginatinib hydrochloride(NS-018 hydrochloride) is highly active against JAK2 with a 50% Inhibition (IC(50)) of < 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 ant Proliferative activity against cell lines expressing a constitutively activated JAK2 (the JAK2V617F or MPLW515L mutations o the TEL-JAK2 fusion gene; IC(50 = 1-120 n), but showed only minimal cytotoxicity against most Other hematopoietic cell lines without a constitutively activated JAK. Read more...

Storage & Handling

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Storage	Pure form: -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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bioavailable, Ilginatinib, Ilginatinib hydrochloride, Ilginatinib Hydrochloride, Janus kinase, JAK, JAK2, JAK1, JAK3, inhibit, NS018, NS-018, NS018 Hydrochloride, NS-018 Hydrochloride, NS-018 hydrochloride, NS 018, NS 018 Hydrochloride, orally, Inhibitor, Tyrosine Kinases, Tyk2, TyrosineKinases

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Compound Identifiers

PubChem CID

89571724 ↗

Key Properties

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No computed properties available.

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