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HLCL-61 hydrochloride

Cat. No. M10073
HLCL-61 hydrochloride Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 55  USD55 In stock
10mg USD 85  USD85 In stock
25mg USD 145  USD145 In stock
50mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

HLCL-61 hydrochloride is a potent and selective, first-in-class protein arginine methyltransferase 5 (PRMT5) inhibitor. HLCL-61 shows no inhibitory activity against the type I (PRMT1 and PRMT4) and type II (PRMT7) PRMT family members. HLCL-61 hydrochloride reduces cells growth at dose-dependent manner with IC50s of 14.12, 16.74, 6.3, 8.72 μM for MV4-11 cells, THP-1 cells, FLT3-WT blast, and FLT3-ITD blast, respectively.

Chemical Information
Molecular Weight 380.91
Formula C23H24N2O.HCl
CAS Number 1158279-20-9
Solubility (25°C) DMSO 49 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] S S Tarighat, et al. Leukemia. The dual epigenetic role of PRMT5 in acute myeloid leukemia: gene activation and repression via histone arginine methylation

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  Catalog
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