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A-1210477

Cat. No. M4932
A-1210477 Structure
Synonym:

A1210477

Size Price Availability Quantity
10mM*1mL USD 160  USD160 In stock
5mg USD 90  USD90 In stock
10mg USD 140  USD140 In stock
25mg USD 290  USD290 In stock
50mg USD 520  USD520 In stock
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Quality Control
Biological Activity

A-1210477 causes a dose-dependent reduction in the amount of BIM co-immunoprecipitated with MCL-1, with an IC50 in the low-μM range. A-1210477 inhibits MCL-1-NOXA interactions with an IC50 of approximately 1 μM, while having no effect on BCL-2-BIM or BCL-XL-BCL-XS interactions measured in the same cell background. A-1210477 binds to MCL-1 selectively and with sufficient affinity to disrupt MCL-1-BIM complexes in living cells. A-1210477 induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines demonstrated to be MCL-1 dependent by BH3 profiling or siRNA rescue experiments.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 850.04
Formula C46H55N7O7S
CAS Number 1668553-26-1
Purity 99.86%
Solubility DMSO 3 mg/mL warmed
Storage at -20°C
References

[1] Bruncko M,et.al. J Med Chem. Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.

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