2. Apoptosis Metabolic Enzyme/Protease
  3. Apoptosis Isocitrate Dehydrogenase (IDH)
  4. IDH1 Inhibitor 9

IDH1 Inhibitor 9 (compound 11S) is a potent IDH1 inhibitor with IC50 values of 124.4, 95.7 nM for IDH1 R132H, IDH1 R132C, respectively. IDH1 Inhibitor 9 induces apoptosis and cell cycle arrest at the S phase. IDH1 Inhibitor 9 shows anti-tumor activity.

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IDH1 Inhibitor 9 Chemical Structure

IDH1 Inhibitor 9 Chemical Structure

CAS No. : 3037967-71-5

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Description

IDH1 Inhibitor 9 (compound 11S) is a potent IDH1 inhibitor with IC50 values of 124.4, 95.7 nM for IDH1 R132H, IDH1 R132C, respectively. IDH1 Inhibitor 9 induces apoptosis and cell cycle arrest at the S phase. IDH1 Inhibitor 9 shows anti-tumor activity[1].

IC50 & Target[1]

R132H IDH1

124.4 nM (IC50)

R132C IDH1

95.7 nM (IC50)

In Vitro

IDH1 Inhibitor 9 (compound 11S) (2, 4, 8, 10 µM) induces apoptosis and cell cycle arrest at the S phase in a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

IDH1 Inhibitor 9 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HT-1080 cells
Concentration: 2, 4, 8 µM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HT-1080 cells
Concentration: 2, 4, 8, 10 µM
Incubation Time: 24 h
Result: Induced cell cycle arrest at the S phase with the percentage of cells in the S phase ranged from 22.4 to 51.6 % with increasing concentrations from 2 to 10 μM.
In Vivo

IDH1 Inhibitor 9 (20, 40 mg/kg; i.p.; every 2 days for 8 days) shows anti-tumor activity for IDH1 mutant cancer model[1].
Pharmacokinetic Parameters (SD rats)[1].

Parameters iv (0.5 mg/kg) po (5 mg/kg)
T1/2 (h) 1.46 ± 0.12 2.13 ± 0.18
Tmax (h) 0.03 ± 0.00 0.19 ± 0.00
Cmax (ng/mL) 766.5 ± 143.1 478 ± 76
AUC(0-t) (hr* ng/mL) 236 ± 283.0 369.7 ± 93.2
CL (mL/h/kg) 1637 ± 212 10103 ± 3310
F % - 16.8 ± 4.7

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4-5 weeks, Female nude mice (HT-1080 xenograft mouse model)[1]
Dosage: 20, 40 mg/kg
Administration: I.p.; every 2 days for 8 days
Result: Suppressed tumor growth without evident loss in body weight.
Molecular Weight

446.54

Formula

C26H30N4O3
CAS No.
SMILES

OC1=CC(OC)=C(C/C=C(C)/C)C=C1C2=NC(N3CCNCC3)=NC(C4=CC=C(O)C=C4)=C2
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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IDH1 Inhibitor 9 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IDH1 Inhibitor 93037967-71-5ApoptosisIsocitrate Dehydrogenase (IDH)apoptosisS phaseanti-tumorHT-1080 cellsInhibitorinhibitorinhibit

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