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Size | Price | Stock |
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100mg | $1980 | To Be Confirmed |
250mg | $3200 | To Be Confirmed |
500mg | $4800 | To Be Confirmed |
Cat #: V4089 CAS #: 1620012-39-6 Purity ≥ 98%
Description: INCB053914 is a novel, potent, selective, and ATP-competitive small molecule pan-inhibitor of PIM (Proviral Integration site of Moloney murine leukemia virus) kinases with IC50 values of 0.24 nM, 30 nM and 0.12 nM for PIM1, PIM2 and PIM3 respectively in biochemical assays.
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Molecular Weight (MW) | 513.52 |
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Molecular Formula | C26H26F3N5O3 |
CAS No. | 1620012-39-6 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: ≥ 10 mg/mLr |
Water: N/Ar | |
Ethanol: N/A | |
SMILES Code | O=C(NC1=CN=C2C(CC[C@H]2O)=C1N3C[C@@H](N)[C@H](O)[C@@H](C)C3)C4=NC(C5=C(F)C=C C=C5F)=C(F)C=C4 |
Synonyms | INCB53914; INCB-53914; INCB 53914; INCB053914; INCB-053914; INCB 053914 |
Protocol | In Vitro | PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib (mean IC50, 4 nM and 27 nM, respectively). Uzansertib (0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM) inhibits the phosphorylation of downstream PIM kinase substrates (p70S6K/S6 and 4E-BP1) in a dose-dependent manner in MOLM-16 (AML), Pfeiffer (DLBCL), and KMS-12-PE/BM (MM) cell lines. Uzansertib inhibits proliferation in all multiple myeloma (MM) cell lines tested, with mean GI50 values ranging from 13.2 nM to 230.0 nM in AML, MM, DLBCL, MCL, and T-ALL cell lines. |
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In Vivo | Uzansertib demonstrates a dose-dependent inhibition of BAD phosphorylation relative to vehicle at 4 hours post dose (MOLM-16 tumors, IC50=70 nM; KMS-12-BM tumors, IC50=145 nM). Uzansertib (25-100 mg/kg; PO; twice a day; for 15 days) inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) . |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.9473 mL | 9.7367 mL | 19.4734 mL | 38.9469 mL |
5mM | 0.3895 mL | 1.9473 mL | 3.8947 mL | 7.7894 mL |
10mM | 0.1947 mL | 0.9737 mL | 1.9473 mL | 3.8947 mL |
20mM | 0.0974 mL | 0.4868 mL | 0.9737 mL | 1.9473 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.