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Dapolsertib

CAT: 0931-T39085-02Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0931-T39085-02Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
1616359-00-2
Target
Pim, FLT, Apoptosis
Related Pathways
Tyrosine Kinase/Adaptors, JAK/STAT signaling, Apoptosis, Angiogenesis, Chromatin/Epigenetic
Purity
0.9961
Bioactivity
Dapolsertib (SEL24-B489) is an orally bioavailable and potent PIM and FLT3-ITD inhibitor, inhibiting PIM1, PIM2, and PIM3, decreasing PIM substrate phosphorylation, and inducing dose-dependent apoptosis in leukemia cells.
Smiles
O=N(=O)C=1C(Br)=C(Br)C=C2C1N=C(N2C(C)C)C3CCNCC3
Molecular Formula
C15H18Br2N4O2
Molecular Weight
446.14
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

Chemical Information

Pim/flt3 kinase inhibitor sel24

Dapolsertib is an orally available inhibitor of PIM family serine/threonine protein kinases and mutant forms of FMS-related tyrosine kinase 3 (FLT3; STK1) with potential antineoplastic activity. Upon oral administration, dapolsertib binds to and inhibits the kinase activities of PIM-1, -2 and -3, and mutant forms of FLT3, which may result in the interruption of the G1/S phase cell cycle transition, an inhibition of cell proliferation, and an induction of apoptosis in tumor cells that overexpress PIMs or express mutant forms of FLT3. FLT3, a tyrosine kinase receptor that is overexpressed or mutated in various cancers, plays a role in signaling pathways that regulate hematopoietic progenitor cell proliferation, and in leukemic cell proliferation and survival. PIM kinases, downstream effectors of many cytokine and growth factor signaling pathways, including the FLT3 signaling pathway, play key roles in cell cycle progression and apoptosis inhibition and may be overexpressed in various malignancies.

CAS Number1616359-00-2
PubChem CID76286825
IUPAC Name5,6-dibromo-4-nitro-2-piperidin-4-yl-1-propan-2-ylbenzimidazole
Molecular FormulaC15H18Br2N4O2
Molecular Weight446.14
XLogP3.5
Topological Polar Surface Area75.7
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count4
Rotatable Bond Count2
Heavy Atom Count23
Formal Charge0
Complexity442
SMILES
CC(C)N1C2=CC(=C(C(=C2N=C1C3CCNCC3)[N+](=O)[O-])Br)Br
InChI
InChI=1S/C15H18Br2N4O2/c1-8(2)20-11-7-10(16)12(17)14(21(22)23)13(11)19-15(20)9-3-5-18-6-4-9/h7-9,18H,3-6H2,1-2H3
InChIKey
UOUBCIJIWDLRGM-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Pim/flt3 kinase inhibitor sel24
CAS: 1616359-00-2
CID: 76286825
Formula: C15H18Br2N4O2
MW: 446.14
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight446.14
XLogP33.5
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count4
Rotatable Bond Count2
Exact Mass445.97760
Monoisotopic Mass443.97965
Topological Polar Surface Area75.7 Ų
Heavy Atom Count23
Formal Charge0
Complexity442
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

Alternative Products

CatalogName
BUP21064-01Dapolsertib

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