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CD38 inhibitor 1

Cat. No. M11546
CD38 inhibitor 1  Structure
Synonym:

compound 78c;CD38-IN-78c;CD38 inhibitor 78c

Size Price Availability Quantity
5mg USD 145  USD145 In stock
10mg USD 245  USD245 In stock
25mg USD 500  USD500 In stock
50mg USD 790  USD790 In stock
100mg USD 1340  USD1340 In stock
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Quality Control & Documentation
Biological Activity

CD38 inhibitor 1 (COMPOUND 78c, CD38-in-78C) was an effective INHIBITOR of CD38, with IC50 of 7.3 nM and 1.9 nM for human AND mouse CD38 respectively.

Chemical Information
Molecular Weight 413.53
Formula C22H27N3O3S
CAS Number 1700637-55-3
Solubility (25°C) DMSO ≥ 60 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] Curt D Haffner, et al. J Med Chem . Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors

[2] Vivek Verma, et al. Nat Immunol. PD-1 blockade in subprimed CD8 cells induces dysfunctional PD-1 + CD38 hi cells and anti-PD-1 resistance

[3] Limo Chen, et al. Cancer Discov. CD38-Mediated Immunosuppression as a Mechanism of Tumor Cell Escape from PD-1/PD-L1 Blockade

[4] Mariana G Tarrag, et al. Cell Metab. A Potent and Specific CD38 Inhibitor Ameliorates Age-Related Metabolic Dysfunction by Reversing Tissue NAD + Decline

[5] Niels W C J van de Donk, et al. Blood. CD38 antibodies in multiple myeloma: back to the future

[6] Antonio Palumbo, et al. N Engl J Med. Daratumumab, Bortezomib, and Dexamethasone for Multiple Myeloma

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Keywords: CD38 inhibitor 1 , compound 78c;CD38-IN-78c;CD38 inhibitor 78c supplier, inhibitors, activators


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