In individual primordial follicles cultured in droplets, Gandotinib at 1 µM for 48 h significantly lowered the proportion of activated follicles, with a greater than 50% reduction compared to DMSO controls. In recombinant protein assays, Gandotinib inhibited JAK2 activity with an IC50 of 6.2 nM. In Ba/F3-JAK2V617F-GFP cells, Gandotinib potently inhibited JAK2V617F signaling, assessed through STAT5 phosphorylation, with IC50=20 nM. [1,2,3]
Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.
Activation of individual primordial follicles
Cell-based study · Individual primordial follicles [1]
Individual primordial follicles were cultured in droplets with Gandotinib at 1 µM for 48 h. The proportion of activated follicles was significantly lower, with a greater than 50% reduction compared to DMSO controls.
Literature-Reported Treatment Conditions
- Treatment concentration
- 1 µM
- Exposure duration
- 48 h
- Method
- cultured in droplets
- Vehicle
- DMSO
Methods and source locations
Compound reported in the paper: Gandotinib
Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.
Results > Tertiary Validation of Hits in Biological Assays. (S47, S48, S49); Materials and Methods > Primordial Follicle In Vitro Culture. (S118)
proportion of activated follicles: proportion of activated follicles; comparator: DMSO controls — Results > Tertiary Validation of Hits in Biological Assays. (S49)
Inhibition of recombinant kinase activity
Biochemical assay · recombinant JAK JH2-JH1 proteins; JAK2 [2]
Effect of inhibitors on kinase activity of recombinant JAK JH2-JH1 proteins was determined using the LANCE Ultra kinase assay. Gandotinib: JAK2 activity inhibition IC50 6.2 nM.
Literature-Reported Treatment Conditions
- Exposure duration
- 5 min interval for 30 min
- Reported limits
- Not stated in the sentences used: dose, route, vehicle, control.
Methods and source locations
Compound reported in the paper: Gandotinib
Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.
Experimental Section > Kinase Assay (S96, S98); Table 1 (T1.h1, T1.h2, T1.r8)
Phosphorylation of the tyrosine kinase substrate: Phosphorylation of the tyrosine kinase substrate — Experimental Section > Kinase Assay (S96); Table 1 (T1.h1, T1.h2, T1.r8)
Signaling inhibition in hematologic cells
Cell-based study · Ba/F3-JAK2V617F-GFP (green fluorescent protein) cells [3]
Gandotinib was evaluated in Ba/F3-JAK2V617F-GFP cells following treatment for 5 h, with STAT5 phosphorylation as the readout. Gandotinib potently inhibited JAK2V617F signaling (IC50=20 nM).
Literature-Reported Treatment Conditions
- Treatment concentration
- 0.001–20 μℳ
- Exposure duration
- 5 h
- Vehicle
- DMSO
- Reported limits
- Not stated in the sentences used: route.
Methods and source locations
Compound reported in the paper: Gandotinib; Compound label in the paper: LY2784544
Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.
Materials and methods > In vitro evaluations > AlphaScreen SureFire assays (S12, S13); Results > Assessment of LY2784544 inhibition of JAK2V617F-induced signaling and cell proliferation (S68, S69)
STAT5 phosphorylation: STAT5 phosphorylation; comparator: vehicle (DMSO) — Results > Assessment of LY2784544 inhibition of JAK2V617F-induced signaling and cell proliferation (S68, S69)
