IDH1 Inhibitor 1

Name: IDH1 Inhibitor 1
Brand: MedChemExpress
SKU: HY-112601
Rating: 4.5 (0 reviews)

Cat. No.: HY-112601 Purity: 99.96%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC₅₀s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1^R132H, IDH1^R132C, and IDH1^WT, respectively. Anticancer activity.

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IDH1 Inhibitor 1 화학구조

CAS No. : 2234285-81-3

사이즈	재고	수량
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 Customer Validation

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View All Isocitrate Dehydrogenase (IDH) Isoform Specific Products:

View All Isoforms

IDH1 IDH2

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

IC50: 0.021 μM (IDH1^R132H), 0.045 μM (IDH1^R132C), and 2.52 μM (IDH1^WT)^[1]

In Vitro

IDH1 Inhibitor 1 (Compound 19) inhibits cellular HCT116-IDH1^R132H/+ with an IC₅₀ of 0.039 μM^[1].

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

In Vivo

IDH1 Inhibitor 1 (Compound 19) inhibits 2-hydroxyglutarate (2-HG) production in a preclinical xenograft tumor model. IDH1 Inhibitor 1 is also profiled in a patient-derived IDH1 mutant HCT116-IDH1^R132H/+ mechanistic xenograft tumor model in mice to evaluate in vivo inhibition of 2-HG production. IDH1 Inhibitor 1, dosed orally at 150 mg/kg, inhibits new 2-HG production^[1].

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

분자량

450.39

화학식

C₂₀H₁₈F₄N₆O₂

CAS No.

2234285-81-3

Appearance

Solid

Color

White to off-white

SMILES

C[C@H](NC1=NC(N2[C@@H](CF)COC2=O)=CC=N1)C(N=C3)=CN3C4=CC=C(C(F)(F)F)C=C4

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

용액&용해도

In Vitro:

DMSO : ≥ 100 mg/mL (222.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2203 mL	11.1015 mL	22.2030 mL
5 mM	0.4441 mL	2.2203 mL	4.4406 mL
10 mM	0.2220 mL	1.1101 mL	2.2203 mL

View the Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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 (5.55 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.55 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.55 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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.96%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (252 KB) HNMR (254 KB) RP-HPLC (223 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[1]. Zhao Q, et al. Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors. ACS Med Chem Lett. 2018 Jun 11;9(7):746-751. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2203 mL	11.1015 mL	22.2030 mL	55.5074 mL
	5 mM	0.4441 mL	2.2203 mL	4.4406 mL	11.1015 mL
	10 mM	0.2220 mL	1.1101 mL	2.2203 mL	5.5507 mL
	15 mM	0.1480 mL	0.7401 mL	1.4802 mL	3.7005 mL
	20 mM	0.1110 mL	0.5551 mL	1.1101 mL	2.7754 mL
	25 mM	0.0888 mL	0.4441 mL	0.8881 mL	2.2203 mL
	30 mM	0.0740 mL	0.3700 mL	0.7401 mL	1.8502 mL
	40 mM	0.0555 mL	0.2775 mL	0.5551 mL	1.3877 mL
	50 mM	0.0444 mL	0.2220 mL	0.4441 mL	1.1101 mL
	60 mM	0.0370 mL	0.1850 mL	0.3700 mL	0.9251 mL
	80 mM	0.0278 mL	0.1388 mL	0.2775 mL	0.6938 mL
	100 mM	0.0222 mL	0.1110 mL	0.2220 mL	0.5551 mL

IDH1 Inhibitor 1 Related Classifications

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 12234285-81-3Isocitrate Dehydrogenase (IDH)Inhibitorinhibitorinhibit

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IDH1 Inhibitor 1

고객리뷰

IDH1 Inhibitor 1 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Isocitrate Dehydrogenase (IDH) Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

IDH1 Inhibitor 1 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

IDH1 Inhibitor 1 Related Classifications

Keywords:

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SAFETY DATA SHEET (SDS)

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