3037967-71-5

Name	IDH1 Inhibitor 9
CAS	3037967-71-5
Molecular Weight	446.54
MOL File	3037967-71-5.mol

Synonyms

IDH1 Inhibitor 9

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Chemical Properties

Boiling point	663.122±65.00 °C(Press: 760.00 Torr)(predicted)
density	1.202±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
pka	7.818±0.50(predicted)

Hazard Information

Uses

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].

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)
T_1/2 (h)	1.46 ± 0.12	2.13 ± 0.18
T_max (h)	0.03 ± 0.00	0.19 ± 0.00
C_max (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

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.

IC 50

R132H IDH1: 124.4 nM (IC₅₀); R132C IDH1: 95.7 nM (IC₅₀)

References

[1] Xu T, et al. Discovery of novel natural-product-derived mutant isocitrate dehydrogenases 1 inhibitors: Structure-based virtual screening, biological evaluation and structure-activity relationship study. Eur J Med Chem. 2024 Jun 17;275:116610. DOI:10.1016/j.ejmech.2024.116610

Supplier

Shanghai Beckham Medical Technology Co., Ltd

Telephone 13816613772

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList16976/0_EN.htm

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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