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Cat. No. M13388
RP-6306 Structure


Size Price Availability Quantity
5mg USD 700  USD700 In stock
10mg USD 1100  USD1100 In stock
25mg USD 2080  USD2080 In stock
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Quality Control & Documentation
Biological Activity

RP-6306 is the first-in-class, highly potent and selective PKMYT1 inhibitor that preferentially kills tumor cells overexpressing CCNE1 and was shown to inhibit the growth of a broad range of CCNE1-amplified tumors in xenograft/PDX preclinical models, both as a single agent and in combination therapy settings. RP-6306 inhibition of Thr14 phosphorylation of CDK1 in HCC1569. 

In vivo, RP-6306 (15, 50, and 300 ppm; oral; daily; for 21 days) results in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth in CCNE1-amplified ovarian xenograft model (OVCAR3).

Chemical Information
Molecular Weight 324.38
Formula C18H20N4O2
CAS Number 2719793-90-3
Form Solid
Solubility (25°C) DMSO 50 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.


[1] Janek Szychowski, et al. J Med Chem. Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306

[2] David Gallo, et al. Nature. CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition

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Keywords: RP-6306, RP6306 supplier, Wee1, inhibitors, activators

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