Mutant IDH1-IN-1 (Synonyms: Agios 135)

Name: Mutant IDH1-IN-1
Brand: MedChemExpress
SKU: HY-12475
Rating: 5.0 (2 reviews)

Cat. No.: HY-12475 Purity: 99.43%: Data Sheet
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Mutant IDH1-IN-1 (Agios 135) is a selective mutant IDH1 inhibitor with activity against both IDH1^R132H and IDH1^R132C. Mutant IDH1-IN-1 reduces the level of 2-hydroxyglutarate (2-HG), stabilizes mutant IDH1 protein, and restores blocked monocyte differentiation. Mutant IDH1-IN-1 can be used in tumor-related research.

For research use only. We do not sell to patients.

CAS No. : 1355326-21-4

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Mutant IDH1-IN-1

: Mutant IDH1-IN-1 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Oct 6;7(1):12758. [Abstract]; Represented western blot of an isothermal dose-response at melting temperature of 59°C demonstrating cellular mIDH1 enzyme thermal stabilization with mIDH1 inhibitors.

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IDH1 IDH2

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

IDH1

In Vitro

Mutant IDH1-IN-1 (30-50 min) potently inhibits purified recombinant IDH1^R132H (with an IC₅₀ of 0.38 µM) and IDH1^R132C (with an IC₅₀ of 0.09 µM), exhibits only weak activity against wild-type IDH1, and shows no activity against wild-type IDH2^[1].
Mutant IDH1-IN-1 (48 h) reduces 2-HG production in HT1080 (IDH1^R132C), SNU1079 (IDH1^R132C), RBE (IDH1^R132S), JJ012 (IDH1^R132G), U87 (IDH1^R132H) and THP-1 (IDH1^R132H) cells without significant cytotoxicity^[1].
Mutant IDH1-IN-1 (0.5 µM; 4 days) rescues doxycycline (HY-N0565)-induced monocytic differentiation of THP-1 (IDH1^R132H) acute myeloid leukemia (AML) cells^[1].
Mutant IDH1-IN-1 (4 days) reduces 2-HG production in 3D tumor spheres of HT1080 (R132C), JJ012 (R132G), and U87 (R132H)^[1].
Mutant IDH1-IN-1 (compound 2) (30 min) potently inhibits the de novo reductive activity of the homodimeric IDH1^R132H, with an IC₅₀ of 0.042 μM^[2].
Mutant IDH1-IN-1 (30 min) potently inhibits the de novo reductive activity of the homodimeric IDH1^R132C, with an IC₅₀ of 0.004 μM^[2].
Mutant IDH1-IN-1 (30 min) inhibits the de novo reductive activity of the heterodimer IDH1^R132H/WT, with an IC₅₀ value of 0.080 μM^[2].
Mutant IDH1-IN-1 (30 min) inhibits the oxidative activity of the heterodimeric R132H/WT IDH1, with an IC₅₀ of 0.143 μM^[2].
Mutant IDH1-IN-1 (30 min) inhibits the oxidative activity of the homodimeric WT/WT IDH1, with an IC₅₀ value of 1.998 μM^[2].

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

Cell Differentiation Assay^[1]

Cell Line:	THP-1 (R132H) AML cells engineered for doxycycline-inducible mIDH1 expression
Concentration:	0.5 µM
Incubation Time:	4 days
Result:	Increased the number of adherent differentiated THP-1 (R132H) cells compared to DMSO control, indicating rescue of the 2-HG-induced differentiation block.

Molecular Weight

498.59

Formula

C₃₀H₃₁FN₄O₂

CAS No.

1355326-21-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(C(C1=C(C)C=CC=C1)N(C(CN2C=NC3=C2C=CC=C3)=O)C4=CC(F)=CC=C4)NC5CCCCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 45 mg/mL (90.25 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	2.0057 mL	10.0283 mL	20.0566 mL
5 mM	0.4011 mL	2.0057 mL	4.0113 mL
10 mM	0.2006 mL	1.0028 mL	2.0057 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, 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.

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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

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.43%

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Data Sheet (281 KB) SDS (254 KB)

COA (257 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Urban DJ, et al. Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays. Sci Rep. 2017;7(1):12758. Published 2017 Oct 6. [Content Brief]

[2]. Deng G, et al. Selective inhibition of mutant isocitrate dehydrogenase 1 (IDH1) via disruption of a metal binding network by an allosteric small molecule. J Biol Chem. 2015;290(2):762-774. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.0057 mL	10.0283 mL	20.0566 mL	50.1414 mL
	5 mM	0.4011 mL	2.0057 mL	4.0113 mL	10.0283 mL
	10 mM	0.2006 mL	1.0028 mL	2.0057 mL	5.0141 mL
	15 mM	0.1337 mL	0.6686 mL	1.3371 mL	3.3428 mL
	20 mM	0.1003 mL	0.5014 mL	1.0028 mL	2.5071 mL
	25 mM	0.0802 mL	0.4011 mL	0.8023 mL	2.0057 mL
	30 mM	0.0669 mL	0.3343 mL	0.6686 mL	1.6714 mL
	40 mM	0.0501 mL	0.2507 mL	0.5014 mL	1.2535 mL
	50 mM	0.0401 mL	0.2006 mL	0.4011 mL	1.0028 mL
	60 mM	0.0334 mL	0.1671 mL	0.3343 mL	0.8357 mL
	80 mM	0.0251 mL	0.1254 mL	0.2507 mL	0.6268 mL

Mutant IDH1-IN-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:

Mutant IDH1-IN-11355326-21-4Agios 135Agios135Agios-135Isocitrate Dehydrogenase (IDH)wild-type IDH22-hydroxyglutarateHT1080 cellsR132H IDH1U87 cellsR132C IDH1wild-type IDH1acute myelogenous leukemiagliomaTHP-1 cellsInhibitorinhibitorinhibit

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Mutant IDH1-IN-1 (Synonyms: Agios 135)

Customer Review

Mutant IDH1-IN-1 Related Antibodies

2 Publications Citing Use of MCE Mutant IDH1-IN-1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Isocitrate Dehydrogenase (IDH) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Mutant IDH1-IN-1 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Mutant IDH1-IN-1 Related Classifications

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Customer Review

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