AP 24534 CAS: 943319-70-8
MF: C29H27F3N6O
MW: 532.57
A Bcr-Abl (Bcr and c-Abl fusion), FGFR, and Flk-1 inhibitor.

AP 24534 (CAS 943319-70-8)

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別名: Ponatinib
アプリケーション: AP 24534 is a Bcr-Abl (Bcr and c-Abl fusion), FGFR, and Flk-1 inhibitor
CAS 番号: 943319-70-8
Purity: ≥98%
Molecular Weight: 532.57
Molecular Formula: C29H27F3N6O
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* Refer to Certificate of Analysis for lot specific data (including water content).

AP 24534 is a small molecule, multi-target kinase inhibitor known to potently inhibit Bcr-Abl (the fusion protein of Bcr and c-Abl), Flk-1(VEGFR2) and FGFR. It also exhibits inhibitory activity against PDGFRα, c-Src and c-Kit. AP 24534 inhibits the proliferation of mutant FLT3-positive cells (IC50 of 13 nM), which inhibits mutant FLT3 phosphorylation (IC50 of 1 nM) and the proliferation of Bcr-Abl1 T315I-positive Ba/F3 cells with an IC50 of 8 nM.

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), ethanol (50 mM), methanol, and water (<1 mg/ml) at 25 °C.
保存方法 :
Store at -20° C
Melting Point :
>160° C (dec.)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.62 (Predicted)
IC50 :
cell lines expressing native BCR-ABL: IC50 = 0.37 nM; cell lines expressing native BCR-ABLT3151: IC50 = 2.0 nM; PDGFRα: IC50 = 1.1 nM; c-Src : IC50 = 5.4 nM; c-Kit : IC50 = 12.5 nM; VEGFR2: IC50 = 1.5 nM; FGFR1: IC50 = 2.2 nM; mutant FLT3 phosphorylation: IC50 = 1 nM; LYN: IC50 = 0.24 nM; ABL kinase domain mutants: IC50 = 0.30 to 0.44 nM; proliferation of mutant FLT3-positive cells: IC50 = 13 nM; proliferation of BCR-ABL1 T315I-positive Ba/F3 cells: IC50 = 8 nM
pK Values :
pKa: 12.99 (Predicted), pKb: 7.54 (Predicted)
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
PubChem CID :
24826799
MDL Number :
MFCD17215203
SMILES :
CC1=C(C=C(C=C1)C(=O)NC2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)C#CC4=CN=C5N4N=CC=C5

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AP 24534 (CAS 943319-70-8)  参考文献

See how others have used AP 24534 (CAS 943319-70-8). Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 29666146  Tamai, TK. et al. 2018. EMBO Mol Med. 10:

Citations 1 to 1 of 1 total
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