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Tocris/Ro 5-3335/4694/10/10 mg

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货号: 4694/10

品牌: Tocris

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Description: Core binding factor inhibitor; attenuates hematopoiesis

Alternative Names: CBFβ-Runx1 inhibitor II

Chemical Name: 7-Chloro-1,3-dihydro-5-(1H-pyrrol-2-yl)-2H-1,4-benzodiazepin-2-one

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC₅₀ = 1.1 μM). Represses RUNX1/CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. Reduces leukemia burden in a mouse model. Attenuates RUNX1-dependent hematopoiesis in zebrafish embryos. Also a Tat antagonist; inhibits HIV-1 replication in vitro.

Technical Data

M. Wt	259.63
Formula	C₁₃H₁₀ClN₃O
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	30195-30-3
PubChem ID	64983
InChI Key	XWNMORIHKRROGW-UHFFFAOYSA-N
Smiles	O=C1CN=C(C3=CC=CN3)C2=C(C=CC(Cl)=C2)N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	25.96	100

Preparing Stock Solutions

The following data is based on the product molecular weight 259.63. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.85 mL	19.26 mL	38.52 mL
5 mM	0.77 mL	3.85 mL	7.7 mL
10 mM	0.39 mL	1.93 mL	3.85 mL
50 mM	0.08 mL	0.39 mL	0.77 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Cunningham et al (2012) Identification of benzodiazepine Ro5-3335 as an inhibitor of CBF leukemia through quantitative high throughput screen against RUNX1-CBF beta interaction. Proc.Natl.Acad.Sci.USA 109 14592 PMID: 22912405

Cupelli et al (1995) The human immunodeficiency virus type 1 Tat antagonist, Ro 5-3335, predominantly inhibits transcription initiation from the viral promoter. J.Virol. 69 2640 PMID: 7884917

Okuda et al (2001) RUNX1/AML1: a central player in hematopoiesis. Int. J. Hematol. 74 252 PMID: 11721959

Keywords: Ro 5-3335, supplier, Ro5-3335, CBF, core, binding, factor, Leukemia, inhibitors, inhibits, runt-related, transcription, factor, 1, RUNX1, acute, myeloid, leukemia, protein, AML1, CBFβ, CBFα, hematopoiesis, HIV-1, replication, antiviral, CBFβ-Runx1, II, CBFbeta-Runx1, inhibitor, II, Antivirals, Other, Transcription, Factors, Other, Transcription, Factors, Tocris Bioscience

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