Camibirstat (Synonyms: FHD-286)

Name: Camibirstat
Brand: MedChemExpress
SKU: HY-144835
Rating: 5.0 (2 reviews)

Art. -Nr.: HY-144835 Reinheit: 98.79%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

FHD-286 is a selective, oral inhibitor of SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor. FHD-286 has the potential for the research of BAF (BRG1/BRM-associated factor)-related disorders such as acute myeloid leukemia.

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CAS. Nr. : 2671128-05-3

Größe	Verfügbarkeit	Menge
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
1 mg	Auf Lager	Estimated Time of Arrival: December 31
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
1 g	Auf Lager	Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Camibirstat

Cell Imaging/Staining

Flow Cytometry

Cell Proliferation/Viability Assay

: Camibirstat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Mar 29.; HeLa cells were pre-treated with or without 1 μM FHD286 for two hours. Laser microirradiation was performed to examine the localization of SMARCA2, SMARCC1 and SMARCD1.

: Camibirstat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Mar 29.; Lacking the enzymatic activities of SMARCA2/4 extends the accumulation of γH2AX, RNF8 and BRCA1. HeLa cells were pre-treated with or without FHD286 (1 μM) or Compound 14 (1 μM) for two hours followed by 5 Gy of IR. Following the indicated recovery time, the foci of γH2AX, RNF8 and BRCA1 were examined by IF.

: Camibirstat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Mar 29.; HR efficacy was examined by GFP reporter assays. U2OS cells with DR-GFP insertion were pretreated with or without FHD286 (1 μM) or Compound 14 (1 μM). I-SceI were expressed to induce DSBs. GFP positive populations were calculated by flowcytometry.

: Camibirstat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Mar 29.; 1000 cells were seeded in each well, and treated with indicated doses of FHD286 and/or olaparib. Colony formation was examined at Day 14 with 0.1% crystal violet staining. Statistical analyses were shown in the lower panel.

: Camibirstat purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Mar 29.; HeLa cells were pre-treated with or without FHD286 (1 μM) or Compound 14 (1 μM) for two hours followed by 5 Gy of IR. Foci formation of RAD51, SMARCA2 were examined.

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

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Beschreibung

In Vitro

FHD-286 (10 to 100 nM) for 7 days induces differentiation followed by loss of viability of AML cell lines and PD AML cells with MLL rearrangement (r), mutant (mt) NPM1 and chromosome 3q26 lesions (with EVI1 overexpression). Treatment with FHD-286 causes whole-genome, concordant, up- or down-regulations in ATAC-Seq peaks and RNA-Seq-determined mRNA expressions of specific loci, associated with significant reduction in the gene-sets of targets of MYC, mTORC1, E2F, Interferon-gamma, IL6-JAK-STAT3, as well as of inflammatory response and oxidative phosphorylation genes. QPCR analyses determined significant reduction in mRNA expression of MYC, SPI1 and BCL2 genes. Mass spectrometry on AML cell lysates treated with FHD-286 showed log2 fold-reductions in c-Myc, SPI1, MEF2C, KMT2C and CDK4 (in MOLM13) and in EVI1, c-Myb, CDK6 and c-Myc (in AML191) cells^[1].

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

In Vivo

FHD-286 (1.5 mg/kg; oral administration; for 10 days) increases in IFNγ and Th1-type chemokine CXCL10 levels^[2].

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

Animal Model:	B16F10 tumor-bearing mice^[2]
Dosage:	1.5 mg/kg
Administration:	Oral administration; for 10 days
Result:	Increased in IFNγ and Th1-type chemokine CXCL10 levels.

Klinische Studie

Molekulargewicht

562.66

Formel

C₂₄H₃₀N₆O₆S₂

CAS. Nr.

2671128-05-3

Appearance

Solid

Color

Off-white to light yellow

SMILES

COC[C@@H](C(NC1=NC(C2=CC=CC(N3C[C@@H](O[C@@H](C3)C)C)=N2)=CS1)=O)NC(C4=CN(C=C4)S(C)(=O)=O)=O

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (444.32 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	1.7773 mL	8.8864 mL	17.7727 mL
5 mM	0.3555 mL	1.7773 mL	3.5545 mL
10 mM	0.1777 mL	0.8886 mL	1.7773 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.

Molaritätsrechner
Verdünnungsrechner

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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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).

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.

Reinheit & Dokumentation

Purity: 98.79%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (249 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

Verweise

[1]. Warren C. Fiskus, et al. Abstract 1140: Pre-clinical efficacy of targeting BAF complexes through inhibition of the dual ATPases BRG1 and BRM by FHD-286 in cellular models of AML. Cancer Res (2023) 83 (7_Supplement): 1140.

[2]. Kana Ichikawa, et al. Synergistic efficacy of the BRM/BRG1 ATPase inhibitor, FHD-286, and anti-PD-1 antibody in mouse syngeneic tumor models.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.7773 mL	8.8864 mL	17.7727 mL	44.4318 mL
	5 mM	0.3555 mL	1.7773 mL	3.5545 mL	8.8864 mL
	10 mM	0.1777 mL	0.8886 mL	1.7773 mL	4.4432 mL
	15 mM	0.1185 mL	0.5924 mL	1.1848 mL	2.9621 mL
	20 mM	0.0889 mL	0.4443 mL	0.8886 mL	2.2216 mL
	25 mM	0.0711 mL	0.3555 mL	0.7109 mL	1.7773 mL
	30 mM	0.0592 mL	0.2962 mL	0.5924 mL	1.4811 mL
	40 mM	0.0444 mL	0.2222 mL	0.4443 mL	1.1108 mL
	50 mM	0.0355 mL	0.1777 mL	0.3555 mL	0.8886 mL
	60 mM	0.0296 mL	0.1481 mL	0.2962 mL	0.7405 mL
	80 mM	0.0222 mL	0.1111 mL	0.2222 mL	0.5554 mL
	100 mM	0.0178 mL	0.0889 mL	0.1777 mL	0.4443 mL

Camibirstat 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:

Camibirstat2671128-05-3FHD-286FHD286FHD 286Oxidative PhosphorylationEpigenetic Reader DomainInhibitorinhibitorinhibit

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Camibirstat (Synonyms: FHD-286)

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Camibirstat Related Antibodies

2 Publications Citing Use of MCE Camibirstat

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biologische Aktivität

Reinheit & Dokumentation

Verweise

Kundenbewertung

Camibirstat Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Camibirstat Related Classifications

Keywords:

Ihre kürzlich angesehenen Produkte:

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