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Indisulam

Cat. No. M8477
Indisulam Structure
Size Price Availability Quantity
5mg USD 75  USD75 In stock
10mg USD 100  USD100 In stock
25mg USD 170  USD170 In stock
50mg USD 265  USD265 In stock
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Quality Control & Documentation
Biological Activity

Indisulam is a carbonic anhydrase inibitor and Antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition.

Chemical Information
Molecular Weight 385.85
Formula C14H12ClN3O4S2
CAS Number 165668-41-7
Form Solid
Solubility (25°C) DMSO: 20 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] Dirksen E Bussiere, et al. Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex

[2] Claudiu T Supuran. Indisulam: an anticancer sulfonamide in clinical development

[3] Jiaqi Lu, et al. Proximity Labeling, Quantitative Proteomics, and Biochemical Studies Revealed the Molecular Mechanism for the Inhibitory Effect of Indisulam on the Proliferation of Gastric Cancer Cells

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Keywords: Indisulam supplier, PROTAC, inhibitors, activators


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