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Chemical Structure| 1429180-08-4 Chemical Structure| 1429180-08-4

Structure of Mutant IDH1 inhibitor
CAS No.: 1429180-08-4

Chemical Structure| 1429180-08-4

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Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.

Synonyms: Mutant IDH1 inhibitor

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Product Details of Mutant IDH1 inhibitor

CAS No. :1429180-08-4
Formula : C25H34N6O3
M.W : 466.58
SMILES Code : CC(C)[C@@H](COC1=O)N1C2=NC(N[C@@H](C)C3=CC=C(CN4CCN(C(C)=O)CC4)C=C3)=NC=C2
Synonyms :
Mutant IDH1 inhibitor
MDL No. :MFCD28167739

Safety of Mutant IDH1 inhibitor

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
TF-1 cells 500 nM To assess the transforming ability of IDH1 R132H/D279N double mutant in TF-1 cells and its sensitivity to ivosidenib. Results showed that IDH1 R132H/D279N could induce cytokine-independent proliferation in TF-1 cells and was resistant to ivosidenib. PMC9440204
Human chondrosarcoma cells 82.5 μM 4 days To evaluate the effect of CP-91149 on cell apoptosis, results showed increased TUNEL-positive cells, indicating increased apoptosis. PMC10592452
Human chondrosarcoma cells 82.5 μM 18 h To evaluate the effect of CP-91149 on cell proliferation, results showed reduced BrdU incorporation, indicating inhibition of cell proliferation. PMC10592452
Human chondrosarcoma cells 82.5 μM 96 h To evaluate the effect of CP-91149 on cell viability, results showed significant reduction in cell viability. PMC10592452

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Patient-derived xenograft model Intraperitoneal injection 50 mg/kg 5 days a week for 2 weeks To evaluate the effect of CP-91149 on tumor growth, results showed significant reduction in tumor size, tumor weight, and tumor volume, and reduced BrdU incorporation, indicating inhibition of cell proliferation. PMC10592452

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.72mL

2.14mL

1.07mL

21.43mL

4.29mL

2.14mL

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