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MYCi975 (Nuc-0200975) is an orally active MYC inhibitor that disrupts MYC/MAX interactions, promotes MYC T58 phosphorylation and MYC degradation, and impairs myC-driven gene expression. MYCi975 (NUC-0200975) has strong anti-tumor effect and good tolerance, increasing tumor immune cell infiltration and enhancing tumor sensitivity against PD1 immune studies.
| 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.
| Molecular Weight | 561.3 |
| Formula | C25H16Cl2F6N2O2 |
| CAS Number | 2289691-01-4 |
| Purity | >99% |
| Solubility | DMSO ≥ 60 mg/mL |
| Storage | at -20°C |
| Related c-Myc Products |
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| VPC-70619
Vpc-70619 is a potent oral active n-myC inhibitor. Vpc-70619 inhibits the binding of n-MyC-Max complex to DNA e-box and exhibits strong inhibitory activity against N-MyC-dependent cell lines and high bioavailability for oral and intrabitoneal administration. |
| ML327
ML327 is a blocker of MYC, which mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition. |
| 10074-G5
10074-G5 is a c-Myc/Max interaction inhibitor, which binds to a different specific binding site (region) of C-Myc than 10054-F4. |
| 10058-F4
10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. |
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