2. Metabolic Enzyme/Protease
  3. Isocitrate Dehydrogenase (IDH)
  4. Safusidenib

Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively.

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Safusidenib Chemical Structure

Safusidenib Chemical Structure

CAS No. : 1898206-17-1

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Based on 1 publication(s) in Google Scholar

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Safusidenib Related Antibodies

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Description

Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma[1]. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively[2].

IC50 & Target

IDH1

 

In Vitro

Safusidenib (DS-1001b) impairs the proliferation of IDH1-mutated chondrosarcoma cell lines and decreases 2-HG levels[1].
Safusidenib impairs the proliferation of IDH1 mutant chondrosarcoma cell lines in a dose-dependent manner, whereas Safusidenib has little effect on the proliferation of the IDH wild-type cell lines OUMS27 and NDCS-1; GI50 values for JJ012, L835, OUMS27, and NDCS-1 cells are 81?nM (day 14), 77?nM (6 weeks), >10?μM (day 10), and >10?μM (day 10), respectively[1].
Safusidenib (1, and 10?μM; for 6 weeks) markedly upregulates SOX9, a key regulator of chondrocyte differentiation, at the protein level[1].
Safusidenib (1 μM) significantly upregulates CDKN1C at the protein level[1].
Safusidenib (DS-1001b) exhibits activity against IDH1 or IDH2 enzymes with IC50s of 8.4, 11, and 180 nM for IDH1R132H, IDH1R132C, and IDH1WT in assays conducted with a 2-hour preincubation step[2].

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

Safusidenib Related Antibodies

Cell Proliferation Assay[1]

Cell Line: The IDH1 mutant cell lines JJ012 and L835 cells
Concentration: 0.1, 1, and 10 μM
Incubation Time: 0, 3, 6, 9, 12, and 15 days
Result: Impaired proliferation in both cell lines in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: L835 cells
Concentration: 0, 1, and 10 μM
Incubation Time: 6 weeks
Result: Markedly upregulated SOX9 at the protein level.
In Vivo

Safusidenib (DS-1001b) has antineoplastic activity in JJ012 xenografts. Continuous administration of Safusidenib (mixed with sterilized pellet food and fed continuously for 6 weeks) impairs tumor growth in xenograft mice[1].

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

Animal Model: NOD-SCID bearing JJ012 xenograft[3]
Dosage: Mixed with sterilized pellet food (CRF-1; Oriental Yeast) and fed ad libitum for 6 weeks. Mixed with sterilized pellet food (CRF-1; Oriental Yeast) and fed ad libitum for 6 weeks.
Administration: Fed continuously starting at 3 weeks
Result: Continuous administration significantly impaired tumor growth in JJ012 xenograft mice.
Clinical Trial
Molecular Weight

535.78

Formula

C25H18Cl3FN2O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1C2=CC=CC(/C=C/C(O)=O)=C2C(C)=C1)C3=C(C(C)(F)C)ON=C3C4=C(C=C(C=C4Cl)Cl)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (186.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8664 mL 9.3322 mL 18.6644 mL
5 mM 0.3733 mL 1.8664 mL 3.7329 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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Volume (final)

V2

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 (4.67 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.67 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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(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:
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% 
+
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%
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).
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.
Purity & Documentation
References

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8664 mL 9.3322 mL 18.6644 mL 46.6609 mL
5 mM 0.3733 mL 1.8664 mL 3.7329 mL 9.3322 mL
10 mM 0.1866 mL 0.9332 mL 1.8664 mL 4.6661 mL
15 mM 0.1244 mL 0.6221 mL 1.2443 mL 3.1107 mL
20 mM 0.0933 mL 0.4666 mL 0.9332 mL 2.3330 mL
25 mM 0.0747 mL 0.3733 mL 0.7466 mL 1.8664 mL
30 mM 0.0622 mL 0.3111 mL 0.6221 mL 1.5554 mL
40 mM 0.0467 mL 0.2333 mL 0.4666 mL 1.1665 mL
50 mM 0.0373 mL 0.1866 mL 0.3733 mL 0.9332 mL
60 mM 0.0311 mL 0.1555 mL 0.3111 mL 0.7777 mL
80 mM 0.0233 mL 0.1167 mL 0.2333 mL 0.5833 mL
100 mM 0.0187 mL 0.0933 mL 0.1866 mL 0.4666 mL
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Safusidenib 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:

Safusidenib1898206-17-1AB-291 DS-1001AB291AB 291DS1001DS 1001DS-1001Isocitrate Dehydrogenase (IDH)orally bioavailablemutant IDH1 inhibitorchondrosarcomaIDH1R132HIDH1R132CInhibitorinhibitorinhibit

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