LY2784544 - ≥98%, high purity , Tyrosine-protein kinase JAK2 inhibitor, CAS No.1229236-86-5, Tyrosine-protein kinase JAK2 inhibitor

Item Number
L126490
Grouped product items
SKUSizeAvailabilityPrice Qty
L126490-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$64.90
L126490-10mg
10mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$107.90
L126490-50mg
50mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$412.90

Basic Description

SynonymsC23H25ClFN7O | 3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine | AKOS037643413 | D10365 | D78334 | Gandotinib;3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpho
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsLY2784544 is identified as being highly selective inhibitor of JAK2 mutant V617F and has advanced into human clinical trials for the treatment of several myeloproliferative disorders.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionTyrosine-protein kinase JAK2 inhibitor
Note卖完停产,不再备货
Product Description

LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.
A selective inhibitor of JAK2 mutant V617F.

Product Properties

ALogP3.8

Associated Targets(Human)

JAK3 Tclin Tyrosine-protein kinase JAK3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
AURKA Tchem Aurora kinase A (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK2 Tclin Tyrosine-protein kinase JAK2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK3 Tclin Tyrosine-protein kinase JAK3 (8349 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TYK2 Tclin Tyrosine-protein kinase TYK2 (5029 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
LIMK1 Tchem LIM domain kinase 1 (2329 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
LIMK2 Tchem LIM domain kinase 2 (949 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SIRT6 Tchem NAD-dependent protein deacetylase sirtuin-6 (671 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
LIMK2 Tchem LIM domain kinase 1/2 (20 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BaF3 (4657 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 3-[(4-chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholin-4-ylmethyl)imidazo[1,2-b]pyridazin-6-amine
INCHI InChI=1S/C23H25ClFN7O/c1-14-9-21(29-28-14)27-22-11-17(13-31-5-7-33-8-6-31)23-26-15(2)20(32(23)30-22)10-16-3-4-18(24)12-19(16)25/h3-4,9,11-12H,5-8,10,13H2,1-2H3,(H2,27,28,29,30)
InChi Key SQSZANZGUXWJEA-UHFFFAOYSA-N
Canonical SMILES CC1=CC(=NN1)NC2=NN3C(=C(N=C3C(=C2)CN4CCOCC4)C)CC5=C(C=C(C=C5)Cl)F
Isomeric SMILES CC1=CC(=NN1)NC2=NN3C(=C(N=C3C(=C2)CN4CCOCC4)C)CC5=C(C=C(C=C5)Cl)F
PubChem CID 46213929
Molecular Weight 469.95

Certificates

Certificate of Analysis(COA)

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Lot NumberCertificate TypeDateItem
J1521094Certificate of AnalysisMay 10, 2023 L126490

Chemical and Physical Properties

SolubilityDMSO 94 mg/mL (200.02 mM); Water <1 mg/mL (<1 mM); Ethanol 9 mg/mL (19.15 mM)

Related Documents

References

1. Ma L, Clayton JR, Walgren RA, Zhao B, Evans RJ, Smith MC, Heinz-Taheny KM, Kreklau EL, Bloem L, Pitou C et al..  (2013)  Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F..  Blood Cancer J,  (13): (e109).  [PMID:23584399] [10.1021/op500134e]
2. Berdeja J, Palandri F, Baer MR, Quick D, Kiladjian JJ, Martinelli G, Verma A, Hamid O, Walgren R, Pitou C et al..  (2018)  Phase 2 study of gandotinib (LY2784544) in patients with myeloproliferative neoplasms..  Leuk Res,  71  (13): (82-88).  [PMID:30025280] [10.1021/op500134e]

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