2. Apoptosis Metabolic Enzyme/Protease
  3. Apoptosis Isocitrate Dehydrogenase (IDH) NAMPT
  4. Mutant IDH1/NAMPT-IN-1

Mutant IDH1/NAMPT-IN-1 (Compound 23h) is a dual inhibitor of mutant isocitrate dehydrogenase 1 (mutant IDH1) (IC50=14.93 nM) and nicotinamide phosphoribosyltransferase (NAMPT) (IC50=12.56 nM). Mutant IDH1/NAMPT-IN-1 can induce apoptosis. Mutant IDH1/NAMPT-IN-1 crosses the blood-brain barrier effectively.

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Mutant IDH1/NAMPT-IN-1 Chemical Structure

Mutant IDH1/NAMPT-IN-1 Chemical Structure

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Mutant IDH1/NAMPT-IN-1 Related Antibodies

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Description

Mutant IDH1/NAMPT-IN-1 (Compound 23h) is a dual inhibitor of mutant isocitrate dehydrogenase 1 (mutant IDH1) (IC50=14.93 nM) and nicotinamide phosphoribosyltransferase (NAMPT) (IC50=12.56 nM). Mutant IDH1/NAMPT-IN-1 can induce apoptosis. Mutant IDH1/NAMPT-IN-1 crosses the blood-brain barrier effectively[1].

IC50 & Target[1]

IDH1

14.93 nM (IC50)

In Vitro

Mutant IDH1/NAMPT-IN-1 (0.5-2 μM; 48 h) is able to dose-dependently reduce 2-HG levels in U87 MG-IDH1R132H cells[1].
Mutant IDH1/NAMPT-IN-1 shows antiproliferative activity against U87 MG IC50=1.26 μM (24 h), 0.77 μM (48 h), 0.42 μM (72 h). Antiproliferative activity against U87 MG-IDH1R132H IC50=0.89 μM (24 h), 0.47 μM (48 h), 0.32 μM (72 h)[1].
Mutant IDH1/NAMPT-IN-1 (0.5 μM; 6 h) improves the thermal stability of NAMPT and IDH1R132H in U87 MG-IDH1R132H cells[1].
Mutant IDH1/NAMPT-IN-1 (0.1-2 μM; 48 h) dose-dependently induces apoptosis in U87 MG-IDH1R132H cells[1].

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

Mutant IDH1/NAMPT-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: U87 MG-IDH1R132H
Concentration: 0.1 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
Result: The apoptosis rate at the concentration of 2 μM was significantly higher than that of the combined group of AG-120 (HY-18767) and FK866 (HY-50876).

Western Blot Analysis[1]

Cell Line: U87 MG-IDH1R132H
Concentration: 0.5 μM
Incubation Time: 6 h
Result: Reduced the expression levels of IDH1R132H, downstream protein TET2, and NAMPT, as well as the upstream protein NAPRT. Decreased the expression of H3K4me3 and H3K27me3.
In Vivo

Mutant IDH1/NAMPT-IN-1 (i.v.; 10-40 mg/kg; twice daily for 35 days) inhibits tumor growth in a dose-dependent manner in BALB/c nude mice[1].
Mutant IDH1/NAMPT-IN-1 (i.v.;400 mg/kg; single dose) is safe to administer in ICR mice[1].


Pharmacokinetic Analysis in SD rats[1]

Route Dose (mg/kg) t1/2 (h) Cmax (ng/mL) Tmax (h) AUC0-t (ng·h/mL) AUC0−∞ (ng·h/mL) Cl ((L/h)/kg) F (%)
i.v. 1 1.16 ± 0.08 4065.66 ± 565.86 0.033 1933.17 ± 131.71 1944.08 ± 132.42 0.26 ± 0.02 /
p.o. 10 2.06 ± 0.29 866.57 ± 225.07 0.75 919.04 ± 40.19 921.26 ± 40.82 / 4.75%

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

Animal Model: BALB/c nude mice[1]
Dosage: 10, 20, and 40 mg/kg
Administration: i.v.; twice daily for 35 days
Result: Median survival times were 25.5, 30.5, and 34 days for the low, middle, and high dose groups, respectively.
40 mg/kg group significantly prolonged survival time in mice and showed superior efficacy compared to FK866 (HY-50876) and IDH305 (HY-104036).
Alleviated weight loss in mice.
Molecular Weight

556.59

Formula

C30H29FN6O4
Unlabeled CAS

SMILES

C[C@@H](C1=CC=C(C=C1)C2=CC=C(C=C2)NC(COC3=CC=CN=C3)=O)NC4=NC(N5[C@H](COC5=O)[C@H](C)F)=CC=N4
Shipping

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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Mutant IDH1/NAMPT-IN-1 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:

Mutant IDH1/NAMPT-IN-1ApoptosisIsocitrate Dehydrogenase (IDH)NAMPTNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorDual InhibitorBrain-PenetrantcancerBALB/c nude miceInhibitorinhibitorinhibit

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