XL228 potently inhibits the tyrosine kinases IGF1R (IC50 = 1.6 nM)

XL228 – 25 mg

Brand:
Cayman
CAS:
898280-07-4
Storage:
-20
UN-No:
Non-Hazardous - /

XL228 potently inhibits the tyrosine kinases IGF1R (IC50 = 1.6 nM) and FGFR1-3 (IC50 50 = 6.1 nM), which mediates metastasis.{33639,33640} It also inhibits the non-receptor tyrosine kinases BCR-ABL (IC50 = 1.4 nM) and Aurora A (IC50 = 3.1 nM), associated with chronic myelogenous leukemia. XL228 showed promising preliminary results in a Phase 1 clinical trial for patients with chronic myelogenous leukemia or Philadelphia-chromosome-positive acute lymphocytic leukemia but the trial was terminated early.{33640}  

 

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Description

XL228 potently inhibits the tyrosine kinases IGF1R (IC50 = 1.6 nM), FGFR1-3 (IC50 50 = 6.1 nM), BCR-ABL (IC50 = 1.4 nM), and Aurora A (IC50 = 3.1 nM)

Formal name: N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-[[3-(1-methylethyl)-5-isoxazolyl]methyl]-6-(4-methyl-1-piperazinyl)-2,4-pyrimidinediamine

Synonyms: 

Molecular weight: 437.5

CAS: 898280-07-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Abl Family & Bcr-Abl||Product Type|Biochemicals|Kinase Inhibitors|Aurora||Product Type|Biochemicals|Kinase Inhibitors|IGF-1R/InsR Family||Product Type|Biochemicals|Kinase Inhibitors|SRC Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Abl family & Bcr-Abl Signaling||Research Area|Cancer|Cell Signaling|Aurora Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Cell Signaling|SRC Family Signaling

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