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Chemical Structure| 819812-04-9 Chemical Structure| 819812-04-9

Structure of KW-2478
CAS No.: 819812-04-9

Chemical Structure| 819812-04-9

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KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM.

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Product Details of KW-2478

CAS No. :819812-04-9
Formula : C30H42N2O9
M.W : 574.66
SMILES Code : O=C(N(CCOC)CCOC)CC1=C(C(C2=CC=C(OCCN3CCOCC3)C(OC)=C2)=O)C(O)=CC(O)=C1CC
MDL No. :MFCD21609267
InChI Key :VFUXSYAXEKYYMB-UHFFFAOYSA-N
Pubchem ID :23116322

Safety of KW-2478

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of KW-2478

DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
32DP-T315I cells 0.6138 µM 48h KW-2478 showed strong inhibition on BCR/ABL-positive cells (32DP-T315I). Exp Hematol Oncol. 2022 May 27;11(1):33
32DP cells 0.639 µM 48h KW-2478 showed strong inhibition on BCR/ABL-positive cells (32DP). Exp Hematol Oncol. 2022 May 27;11(1):33
SUP-B15 cells 1.166 µM 48h KW-2478 showed strong inhibition on BCR/ABL-positive cells (SUP-B15). Exp Hematol Oncol. 2022 May 27;11(1):33
KCL-22 cells 5.473 µM 48h KW-2478 showed strong inhibition on BCR/ABL-positive cells (KCL-22). Exp Hematol Oncol. 2022 May 27;11(1):33
THP-1 cells 29.07 µM 48h KW-2478 showed weaker inhibition on BCR/ABL-negative cells (THP-1). Exp Hematol Oncol. 2022 May 27;11(1):33
KG-1a cells 37.06 µM 48h KW-2478 showed weaker inhibition on BCR/ABL-negative cells (KG-1a). Exp Hematol Oncol. 2022 May 27;11(1):33
K562 cells 5.195 µM (48h), 4.659 µM (72h) 48h and 72h KW-2478 inhibited K562 cell proliferation in a dose- and time-dependent manner. Exp Hematol Oncol. 2022 May 27;11(1):33
Primary MM cells 1 and 2 μmol/L 48 hours KW-2478 enhanced the anti-MM activity of bortezomib, with significant effects in some samples. Blood Cancer J. 2012 Apr;2(4):e68
OPM-2/GFP cells 2.2 to 5 μmol/L 3 hours KW-2478 enhanced bortezomib-induced cell growth inhibition and showed synergistic effects (CI values 0.76 to 0.82). Blood Cancer J. 2012 Apr;2(4):e68
4T1 cells 1 µM 24 hours Evaluate the effect of KW-2478 on 4T1 cells, showing that KW-2478 increased the number of 4T1 cells with aberrant nuclei Biomedicines. 2022 Aug 16;10(8):1988
b.End5 cells 1 µM 24 hours Evaluate the effect of KW-2478 on β-catenin expression in b.End5 cells, showing that KW-2478 increased β-catenin expression at the cell membrane Biomedicines. 2022 Aug 16;10(8):1988
LLC-PK cells 5, 10, 20 μM 24 hours Evaluate the effect of KW-2478 on PDCoV infection, results showed that KW-2478 had no significant inhibitory effect on PDCoV infection J Biol Chem. 2024 Jan;300(1):105536

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID mice CML-like mouse models Intraperitoneal injection 50 mg/kg/day Administered every other day for 3 weeks KW-2478 significantly prolonged mouse lifespan and alleviated disease symptoms and tumor cell infiltration. Exp Hematol Oncol. 2022 May 27;11(1):33
Severe combined immunodeficient mice NCI-H929 subcutaneous xenograft model Intravenous injection KW-2478 50 mg/kg, bortezomib 1 mg/kg Twice weekly for 2 weeks The combination therapy showed synergistic anti-tumor activity without significant body weight loss. Blood Cancer J. 2012 Apr;2(4):e68

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00457782 Multiple Myeloma|Chronic Lymph... More >>ocytic Leukaemia|B-cell Non-Hodgkin's Lymphoma Less << PHASE1 COMPLETED 2025-01-11 St Bartholomew's Hospital, Lon... More >>don, United Kingdom|UCLH, London, United Kingdom|Christie Hospital, Manchester, United Kingdom|Nottingham University NHS Trust, Nottingham, United Kingdom|Cancer Research UK Clinical Centre, Southampton, United Kingdom|Royal Marsden Hospital, Sutton, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.74mL

0.35mL

0.17mL

8.70mL

1.74mL

0.87mL

17.40mL

3.48mL

1.74mL

References

 

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