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BML-277

Cat. No. M5137
BML-277 Structure
Synonym:

Chk2 Inhibitor II

Size Price Availability Quantity
10mM*1mL in DMSO USD 65  USD65 In stock
5mg USD 58  USD58 In stock
10mg USD 88  USD88 In stock
50mg USD 350  USD350 In stock
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Quality Control & Documentation
Biological Activity

BML-277 protects T cells from apoptosis by controlling the response of p53 to radiation-induced DNA breaks. This is suggestive of BML-277's use as an adjuvant for radiation therapy in cancer. BML-277 is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. It has also been found to weakly inhibit 31 other kinases.

Product Citations
Chemical Information
Molecular Weight 363.8
Formula C20H14ClN3O2
CAS Number 516480-79-8
Solubility (25°C) DMSO 55 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Arienti KL,et.al. J Med Chem. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles.

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Keywords: BML-277, Chk2 Inhibitor II supplier, Checkpoint, inhibitors, activators


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