Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other sizes |
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Targets |
HPK1 (IC50 = 2.6 nM); GLK/MAP4K3 (IC50 = 140 nM); IRAK4 (IC50 = 59 nM); Fms/CSFR (IC50 = 3.2 nM ); FLT3 (IC50 = 25.4 nM);AMPKA1 (IC50 = 44.3 nM); cKIT (IC50 = 45.7 nM); MST1(IC50 = 55.1 nM)
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ln Vivo |
In a syngeneic tumor model of colorectal cancer, HPK1-IN-7 (100 mg/kg; p.o.; twice daily for 28 days) exhibits a significant enhancement of anti-PD1 efficacy.
HPK1-IN-7 (compound 24) has a volume of distribution of 4.4 L/kg and a moderate plasma clearance of 43 mL/min/kg. It is administered intravenously to mice at a dose of 1 mg/kg. The AUC0-24h was 19 M•h and the Cmax was 5.3 M following oral administration (20 mg/kg). Based on these pharmacokinetics studies, the calculated oral bioavailability is approximately 100%. |
Animal Protocol |
Animal Model:Mice (MC38 syngeneic tumor model)
Dosage: 100mg/kg Administration: Oral; twice daily for 28 days Result: increased the anti-PD1 treatment's effectiveness, achieving a 100% cure rate as opposed to a 20% cure rate with anti-PD1 alone. |
References |
Molecular Formula |
C24H22N6O4
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Molecular Weight |
458.47
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Exact Mass |
458.17
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Elemental Analysis |
C, 62.87; H, 4.84; N, 18.33; O, 13.96
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CAS # |
2320462-65-3
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Related CAS # |
2320462-65-3;
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Appearance |
Solid powder
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SMILES |
CC1(C2=C(C=CC(=C2)NC3=NC=C(C(=N3)N[C@H]
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InChi Key |
RVSSNRBUPQUIEG-LJQANCHMSA-N
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InChi Code |
InChI=1S/C24H22N6O4/c1-24(2)18-10-15(8-9-16(18)22(32)34-24)27-23-25-11-17(21-30-26-13-33-21)20(29-23)28-19(12-31)14-6-4-3-5-7-14/h3-11,13,19,31H,12H2,1-2H3,(H2,25,27,28,29)/t19-/m1/s1
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Chemical Name |
5-[[4-[[(1S)-2-hydroxy-1-phenylethyl]amino]-5-(1,3,4-oxadiazol-2-yl)pyrimidin-2-yl]amino]-3,3-dimethyl-2-benzofuran-1-one
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Synonyms |
HPK1-IN-7 ; HPK1-IN 7, HPK1-IN7
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~125.0 mg/mL (~272.7 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1812 mL | 10.9058 mL | 21.8117 mL | |
5 mM | 0.4362 mL | 2.1812 mL | 4.3623 mL | |
10 mM | 0.2181 mL | 1.0906 mL | 2.1812 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(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.
Docking of 2 and 3 into HPK1 homology model. ACS Med Chem Lett . 2021 Feb 19;12(3):443-450. td> |
X-ray crystal structure of 24 bound to HPK1 (PDB: 7KAC). ACS Med Chem Lett . 2021 Feb 19;12(3):443-450. td> |