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B02 1290541-46-6

B02 1290541-46-6

CAS No.: 1290541-46-6

B02 (also called RAD51-IN-02)is a potent and specific inhibitor of human RAD51 with an IC50 of 27.4 μM. In many types o
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B02 (also called RAD51-IN-02)is a potent and specific inhibitor of human RAD51 with an IC50 of 27.4 μM. In many types of cancer cells, RAD51 is overexpressed. Chemo- or radio-sensitive cancer cells are enhanced when RAD51 is downregulated by siRNA. B02 induces a heightened sensitivity to various agents that damage DNA and inhibits HR repair in human embryonic kidney (HEK) and breast cancer cells. B02 also makes decitabine-induced apoptosis and DNA damage in MM cells more pronounced”. B02 exhibits a high degree of specificity for RAD51 and does not substantially inhibit RAD54 across a concentration range of 0 to 200 μM.


Physicochemical Properties


Molecular Formula C22H17N3O
Molecular Weight 339.39
Exact Mass 339.137
Elemental Analysis C, 77.86; H, 5.05; N, 12.38; O, 4.71
CAS # 1290541-46-6
Related CAS #
1290541-46-6
PubChem CID 5738263
Appearance Light yellow to yellow solid powder
LogP 4.01
Hydrogen Bond Donor Count 0
Hydrogen Bond Acceptor Count 3
Rotatable Bond Count 4
Heavy Atom Count 26
Complexity 550
Defined Atom Stereocenter Count 0
SMILES

O=C1C2=C([H])C([H])=C([H])C([H])=C2N=C(/C(/[H])=C(\[H])/C2=C([H])N=C([H])C([H])=C2[H])N1C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H]

InChi Key GEKDQXSPTHHANP-OUKQBFOZSA-N
InChi Code

InChI=1S/C22H17N3O/c26-22-19-10-4-5-11-20(19)24-21(13-12-17-9-6-14-23-15-17)25(22)16-18-7-2-1-3-8-18/h1-15H,16H2/b13-12+
Chemical Name

3-benzyl-2-[(E)-2-pyridin-3-ylethenyl]quinazolin-4-one
Synonyms

B02; B-02; B 02; RAD51-IN-02; RAD51-IN 02; RAD51 IN-02; RAD51 Inhibitor B02
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets hRAD51 ( IC50 = 27.4 μM )
ln Vitro

In vitro activity: B02 is a particular inhibitor of human RAD51 recombinase that prevents HR repair in HEK and breast cancer cells and makes them more vulnerable to various agents that damage DNA. Additionally, B02 increases the apoptosis and DNA damage that decitabine causes in MM cells[1]. In the range of concentrations from 0 to 200 μM, B02 does not significantly inhibit RAD54 and exhibits high specificity for RAD51[2]. B02 exhibits physiological effects in both mouse and human cells. B02 suppresses the formation of RAD51 foci in response to DNA damage in human embryonic kidney (HEK) cells, which in turn inhibits DSB repair and DSB-dependent HR. Additionally, B02 may make cancer cells more susceptible to DNA-damaging chemotherapeutic agents[3].
ln Vivo
B02 increases cisplatin's anti-tumor activity in vivo by a considerable amount. In the liver and kidneys, the primary organs involved in detoxification, no observable morphological alterations brought on by B02 have been established[3].
Cell Assay The WST-1 colorimetric cell count assay is used to track the proliferation of MM-cell lines. Approximately 8000 cells/well are seeded in 96-well plates with MM cell lines. After one hour of treatment with or without B02 (10 μM), the cells are treated for a further 72 hours with either vehicle (DMSO) or DOX (20–160 nM). Each well's culture medium receives a 1:10 addition of WST-1 reagent, and the incubation process lasts for four hours at 37°C. With a spectrophotometer, the absorbance at 450 nm is used to estimate the relative cell number.
Animal Protocol
Mice: The solutions of cisplatin and B02 are made up of NS and cremophor/DMSO/NS (1:1:3), respectively, right before injection. B02 (50 mg/kg or as indicated) and cisplatin (4 mg/kg or as indicated) are injected into mice in a combination treatment group. Mice are injected with B02 and NS in the B02 group and cisplatin and B02 vehicle in the cisplatin group. Three hours after the B02 (or its vehicle) injection, cisplatin (or NS) is administered. On days 11, 13, 15, and 17 following tumor cell inoculations, intraperitoneal injections (I.P.) are used to administer all treatments.
References

[1]. Front Oncol . 2014 Oct 30:4:289.

[2]. ACS Chem Biol . 2011 Jun 17;6(6):628-35.

[3]. PLoS One . 2014 Jun 27;9(6):e100993.
Additional Infomation 3-(phenylmethyl)-2-[2-(3-pyridinyl)ethenyl]-4-quinazolinone is a member of quinazolines.

Solubility Data


Solubility (In Vitro)
DMSO: ~67 mg/mL (~197.4 mM)
Water: <1 mg/mL
Ethanol: ~20 mg/mL (~58.9 mM)
Solubility (In Vivo) Solubility in Formulation 1: 10 mg/mL (29.46 mM) in 20% DMSO 20% Cremophor EL + 60% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.
Solubility in Formulation 2: ≥ 2 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.
Solubility in Formulation 3: ≥ 2 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.9465 mL 14.7323 mL 29.4646 mL
5 mM 0.5893 mL 2.9465 mL 5.8929 mL
10 mM 0.2946 mL 1.4732 mL 2.9465 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Is for research use only, not for human use. We do not sell to patients.