Casein Kinase inhibitor A86
CAS No. : 2079069-01-3
| Size | Price | Stock |
|---|---|---|
| 5mg | $280 | In-stock |
| 10mg | $476 | In-stock |
| 25mg | $945 | In-stock |
| 50mg | $1540 | In-stock |
| 100mg | $2380 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-123955 |
| M.Wt: | 344.43 |
| Formula: | C18H25FN6 |
| Purity: | >98 % |
| Solubility: | DMSO : 12.5 mg/mL (ultrasonic;warming;heat to 60°C) |
Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities[1].
In Vitro: Casein Kinase inhibitor A86 is highly effective in inducing leukemia cell apoptosis at 160 nM or lower, mostly in correlation to their capacity to stabilize p53[1].
Casein Kinase inhibitor A86 (0.08-2 μM; 6.5 hours) abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. Casein Kinase inhibitor A86 induces a marked reduction in mRNA expression of MYC and MDM2, yet upregulates the expression of the Wnt targets AXIN2 and CCND1 (Cyclin D1)[1].
In Vivo: Pharmacokinetic studies of the inhibitor Casein Kinase inhibitor A86 at 20 mg/kg reveal rapid oral absorption with a Tmax of 0.2-0.5 hr, Cmax of 1115 ng/mL, T1/2 of 4.3 hr, and area under the curve (AUC) values of 2606 (ng*hr/mL)[1].
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