Cat. No.: HY-104036

IDH-305

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC₅₀= 27 nM (IDH1^R132H), 28 nM (IDH1^R132C), 6.14 µM (IDH1^WT)).

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Pureté: 99.15%
CAS No.: 1628805-46-8
Formule: C₂₃H₂₂F₄N₆O₂
Masse moléculaire:490.45

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

IDH-305 Chemical Structure

CAS No.: 1628805-46-8

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (4)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IDH1

Voir tous les produits spécifiques à Isoform Isocitrate Dehydrogenase (IDH) :

IDH1
IDH2

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	24 nM Compound: 60; IDH305	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell growth by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell growth by MTT assay	[PMID: 37235998]
HCT-116	IC₅₀	25 nM Compound: 60; IDH305	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 5 days by Celltiter-Glo assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 5 days by Celltiter-Glo assay	[PMID: 37235998]
U-87MG ATCC	IC₅₀	0.36 μM Compound: 6; IDH305	Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	0.44 μM Compound: 6; IDH305	Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	0.45 μM Compound: 6; IDH305	Synergistic antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs in presence of FK866 by CCK8 assay Synergistic antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs in presence of FK866 by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	1.04 μM Compound: 6; IDH305	Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	1.69 μM Compound: 6; IDH305	Synergistic antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs in presence of FK866 by CCK8 assay Synergistic antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs in presence of FK866 by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	20.13 μM Compound: 6; IDH305	Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 24 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	3.54 μM Compound: 6; IDH305	Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 38651495]
U-87MG ATCC	IC₅₀	7.57 μM Compound: 6; IDH305	Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against human U-87 MG cells harboring wildtype IDH1 assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 38651495]

In Vitro

IDH-305 inhibits HCT116-IDH1^R132H+/- cells with an IC₅₀ of 24 nM^[1].

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

In Vivo

IDH-305 (30-300 mg/kg; p.o.; twice daily for 21 days) inhibits 2-HG production and 2-HG-dependent tumor growth of an IDH1 mutant PDX melanoma model^[1].

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

Animal Model:

nu/nu mice (HMEX2838-IDH1^R132C+/-PDX model)^[1]
Dosage:

30, 100, 300 mg/kg
Administration:

Oral gavage; twice daily for 21 days
Result:

Resulted in 62-67% 2-HG reduction and significant anti-tumor activity at 100 mg/kg and 97-99% 2-HG reduction and partial tumor regression of 32% at 300 mg/kg.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1628805-46-8
Appearance Solid
Masse moléculaire 490.45
Formule C₂₃H₂₂F₄N₆O₂
Color White to off-white
SMILES

O=C1OC[C@H]([C@@H](F)C)N1C2=NC(N[C@H](C3=CC(C)=C(C4=CC(C(F)(F)F)=NC=C4)C=N3)C)=NC=C2
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Science

Mutant IDH1 inhibition induces dsDNA sensing to activate tumor immunity. [Abstract]

2024 Jul 12;385(6705):eadl6173. PMID: 38991060
Nat Commun

Single-cell multi-omics identifies metabolism-linked epigenetic reprogramming as a driver of therapy-resistant medulloblastoma. [Abstract]

2025 Nov 25;16(1):10470. PMID: 41290646
Nat Chem Biol

Autopalmitoylation of IDH1-R132H regulates its neomorphic activity in cancer cells. [Abstract]

2026 Jan 13. PMID: 41530531
Cancer Res Commun

Mutant Isocitrate Dehydrogenase 1 Sensitizes Intrahepatic Cholangiocarcinoma Cells to MDM2 Inhibitors. [Abstract]

2026 Mar 1;6(3):616-629. PMID: 41747217

Solvant et solubilité

In Vitro:

DMSO : ≥ 150 mg/mL (305.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0389 mL

10.1947 mL

20.3894 mL

5 mM

0.4078 mL

2.0389 mL

4.0779 mL

10 mM

0.2039 mL

1.0195 mL

2.0389 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Cho YS, et al. Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor. ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121. [Content Brief]

[2]. Courtney D DiNardo, et al. A Phase I Study of IDH305 in Patients with Advanced Malignancies Including Relapsed/Refractory AML and MDS That Harbor IDH1R132 Mutations. Blood, 128(22), 1073.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0389 mL	10.1947 mL	20.3894 mL	50.9736 mL
	5 mM	0.4078 mL	2.0389 mL	4.0779 mL	10.1947 mL
	10 mM	0.2039 mL	1.0195 mL	2.0389 mL	5.0974 mL
	15 mM	0.1359 mL	0.6796 mL	1.3593 mL	3.3982 mL
	20 mM	0.1019 mL	0.5097 mL	1.0195 mL	2.5487 mL
	25 mM	0.0816 mL	0.4078 mL	0.8156 mL	2.0389 mL
	30 mM	0.0680 mL	0.3398 mL	0.6796 mL	1.6991 mL
	40 mM	0.0510 mL	0.2549 mL	0.5097 mL	1.2743 mL
	50 mM	0.0408 mL	0.2039 mL	0.4078 mL	1.0195 mL
	60 mM	0.0340 mL	0.1699 mL	0.3398 mL	0.8496 mL
	80 mM	0.0255 mL	0.1274 mL	0.2549 mL	0.6372 mL
	100 mM	0.0204 mL	0.1019 mL	0.2039 mL	0.5097 mL

Keywords

IDH-305

4 Cited Publications

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IDH-305

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Publications Citing Use of MedChemExpress (MCE) IDH-305

Voir tous les produits spécifiques à Isoform Isocitrate Dehydrogenase (IDH)

Activité biologique

Chemical Information

Publications (4)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

IDH-305

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Cancer Metabolism Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

TCA Cycle Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) IDH-305

Voir tous les produits spécifiques à Isoform Isocitrate Dehydrogenase (IDH)

Activité biologique

Chemical Information

Publications (4)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

IDH-305 Related Classifications

Cat. No.: HY-104036