CCT241736

SKU: orb1302867

Description

CCT241736 is an orally active dual inhibitor of FLT3 and Aurora kinases, effective against resistant FLT3 mutants like ITD. This preclinical candidate shows potent activity in vitro and in vivo, supporting its development for acute myeloid leukemia (AML) in both adult and pediatric contexts.

Research Area

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

Key Properties

• CAS Number: 1402709-93-6
• MW: 456.37
• Purity: 99.88% (May vary between batches)
• Formula: C₂₂H₂₃Cl₂N₇
• SMILES: Cc1nn(C)cc1-c1nc2c(N3CCN(Cc4ccc(Cl)cc4)CC3)c(Cl)cnc2[nH]1
• Target: Aurora Kinase|||FLT
• Solubility: H2O:< 0.1 mg/mL (insoluble);10% DMSO+90% Corn Oil:3.3 mg/mL (7.23 mM);DMSO:75 mg/mL (164.34 mM)

Bioactivity

• Target IC50:
  Aurora A:7.5 nM (Kd)|Aurora A:38 nM|FLT3 (D835H):11 nM (Kd)|FLT3:6.2 nM (Kd)|Aurora B:48 nM (Kd)|FLT3 (N841I):16 nM (Kd)|FLT3 (ITD):38 nM (Kd)|FLT3 (R834Q):110 nM (Kd)|FLT3 (K663Q):5.1 nM (Kd)|FLT3 (D835Y):14 nM (Kd)
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• In Vivo:
  UNC2025 was capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, FLT3, Fms like tyrosine kinase 3, Aurora Kinase, AuroraKinase, CCT241736, CCT-241736, CCT 241736, Cluster of differentiation antigen 135, CD135

Compound Identifiers

PubChem CID

71454279