Gandotinib (LY2784544) - Moligand™, 10mM in DMSO , Tyrosine-protein kinase JAK2 inhibitor, CAS No.1229236-86-5, Tyrosine-protein kinase JAK2 inhibitor

CAS: 1229236-86-5 Cat. No.: G409108 Peso molecular: 469.95

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Gandotinib (LY2784544) is a potentJAK2inhibitor withIC50of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.
In vitro

LY2784544 also inhibits IL-3-activated wild type JAK2 with IC50 of 2.26 μM. Similarly in the proliferation assay, LY2784544 shows antiproliferation activity in JAK2 V617F-driven cells with IC50 of 68 nM, compared to 1.36 μM in wild type JAK2-driven cells and 0.94 μM in JAK3-driven cells. Though biochemical assays do not reveal selectivity of LY2784544 for mutant JAK2V617F, LY2784544 shows higher selectivity for inhibition of JAK2-mediated signaling and induction of apoptosis in Ba/F3 cells expressing JAK2V617F than wild-type cells.

In vivo

LY2784544 significantly inhibits STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP xenografts with a Threshold Effective Dose 50 (TED50) of 12.7 mg/kg. LY2784544 also reduces Ba/F3-JAK2 V617F-GFP tumor burden in the JAK2 V617F-induced MPN model with a TED50 of 13.7 mg/kg after oral treatment. LY2784544 has no effect on CD71/Ter119 positive erythroid progenitors in spleens of SCID mice after oral treatment.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Sinónimos

3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1, 2-b]pyridazin-6-amine

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Gandotinib (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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Tyrosine-protein kinase JAK2 inhibitor

Propiedades del producto

• ALogP: 3.8

Nombres e identificadores

• Isómeros SMILES: CC1=CC(=NN1)NC2=NN3C(=C(N=C3C(=C2)CN4CCOCC4)C)CC5=C(C=C(C=C5)Cl)F
• Peso molecular: 469.95
• Reaxy-Rn: 20329925
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20329925&ln=

Objetivos asociados (humanos)

JAK3 Tclin Tyrosine-protein kinase JAK3 (1 Activities)

Discover Target: JAK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKA Tchem Aurora kinase A (1 Activities)

Discover Target: AURKA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

JAK2 Tclin Tyrosine-protein kinase JAK2 (1 Activities)

Discover Target: JAK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 44 mg/mL (198.87 mM); Ethanol: 44 mg/mL (198.87 mM); Water: Insoluble

Referencias

1. Chuchu Xu, Renjun Zhu, Qingfeng Dai, Yaoqing Li, Gengyuan Hu, Kelong Tao, Yuhong Xu, Guangen Xu, Guolin Zhang.  (2025)  TIMP-2 Modulates 5-Fu Resistance in Colorectal Cancer Through Regulating JAK–STAT Signalling Pathway.  JOURNAL OF CELLULAR AND MOLECULAR MEDICINE,  29  (6): (e70470).  [PMID:40118773] [10.1111/jcmm.70470]