Gandotinib

SKU: orb1305233

Description

Gandotinib

Research Area

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

Images & Validation

−

Key Properties

−

CAS Number	1229236-86-5
MW	469.94
Purity	99.86%
Formula	C₂₃H₂₅ClFN₇O
SMILES	C(C=1C=2N(C(CC3=C(F)C=C(Cl)C=C3)=C(C)N2)N=C(NC=4C=C(C)NN4)C1)N5CCOCC5
Target	FGFR,JAK,VEGFR,FLT
Solubility	Ethanol:9 mg/mL (19.15 mM);DMSO:87 mg/mL (185.13 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.02 mM)

Bioactivity

−

Target IC50	AURKA:168 nM\|TRKB:95 nM\|ALK:138 nM\|Tyk2:44 nM\|KDR:109 nM\|JAK2:3 nM\|MAP3K9:299 nM\|FLT3:4 nM\|FGFR3:106 nM\|JAK2 (V617F):0.245 nM(Ki)\|MUSK:147 nM\|FGFR2:32 nM\|JAK3:48 nM\|FLT4:25 nM Read more...
In Vivo	In proliferation assays, LY2784544 exhibits an anti-proliferative effect on JAK2 V617F-driven cells, with an IC50 of 68 nM. It demonstrates a less potent effect on cells driven by wild-type JAK2 and JAK3, with IC50 values of 1356 nM and 940 nM, respectively. LY2784544 also inhibits IL-3-activated wild-type JAK2 with an IC50 of 2.26 μM. Read more...
In Vitro	In severe combined immunodeficient mice, LY2784544 (administered orally) does not affect CD71/Ter119 positive erythroid progenitor cells within the spleen. LY2784544 significantly inhibits STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP xenografts (effective dose 50% [ED50]: 12.7 mg/kg). Additionally, in a JAK2 V617F-induced myeloproliferative neoplasm (MPN) model, LY2784544 (administered orally) reduces the tumor burden of Ba/F3-JAK2 V617F-GFP (ED50: 13.7 mg/kg). Read more...
Cell Research	LY2784544 is dissolved in DMSO and stored, and then diluted with appropriate medium before use. Ba/F3 cells expressing JAK2V617F are placed in RPMI-1640-containing vehicle (DMSO) or LY2784544 (concentration range, 0.001-20 μM) (1×104 cells/96-well). Ba/F3 cells expressing wild-type JAK2 are treated similarly except IL-3 (2 ng/mL) is added. After a 72-hour incubation, cell proliferation is assessed by adding Cell Titer 96 Aqueous One Solution Reagent (20 μL/well). The IC50 for inhibition of cell proliferation is calculated using the GraphPad Prism 4 software. Read more...

Storage & Handling

−

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

−

Vascular endothelial growth factor receptor, VEGFR, FLT3, Fibroblast growth factor receptor, Fms like tyrosine kinase 3, FGFR, Inhibitor, Gandotinib, Janus kinase, JAK, inhibit, JAK2, JAK1, JAK2 (V617F), LY 2784544, LY2784544, LY-2784544, CD135, Cluster of differentiation antigen 135

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

46213929 ↗

Key Properties

−

No computed properties available.

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols

Gandotinib (orb1305233)

Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

No reviews yet

Purity:	>98% (HPLC)
CAS Number:	1229236-86-5
MW:	469.9
Formula:	C₂₃H₂₅ClFN₇O

Gandotinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

LY2784544 [orb1226732]

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

Request a Document

Protocol Information

Gandotinib (orb1305233)

Step 1: Enter information below

Step 2: Enter the in vivo formulation

Available Sizes

Email

UK Office

US Office

CN Office

Distributors