INK 128 (MLN0128) 1224844-38-5
Product Description
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Molecular Weight: 309.33 INK 128 (MLN0128) is a potent and selective mTOR Inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6
and 4EBP1, the downstream substrates of TORC1, and selectively inhibits
AKT phosphorylation at Ser473, the downstream substrate of TORC2.
Furthermore, INK 128 also shows potent inhibition effects on cell lines
resistant to rapamycin and pan-PI3K Inhibitors.
In a ZR-75-1 breast cancer xenograft model, INK 128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day. Daily, oral administration of INK 128 inhibits Angiogenesis and tumor growth in multiplexenograft models.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Chemical Information
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Contact us if you need more details on INK 128 1224844-38-5. We are ready to answer your questions on packaging, logistics, certification or any other aspects about MLN0128 1224844-38-5、1224844-38-5 INK 128. If these products fail to match your need, please contact us and we would like to provide relevant information.
Molecular Weight: 309.33 INK 128 (MLN0128) is a potent and selective mTOR Inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6
and 4EBP1, the downstream substrates of TORC1, and selectively inhibits
AKT phosphorylation at Ser473, the downstream substrate of TORC2.
Furthermore, INK 128 also shows potent inhibition effects on cell lines
resistant to rapamycin and pan-PI3K Inhibitors.
In a ZR-75-1 breast cancer xenograft model, INK 128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day. Daily, oral administration of INK 128 inhibits Angiogenesis and tumor growth in multiplexenograft models.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species | Baboon | Dog | Monkey | Rabbit | Guinea pig | Rat | Hamster | Mouse |
Weight (kg) | 12 | 10 | 3 | 1.8 | 0.4 | 0.15 | 0.08 | 0.02 |
Body Surface Area (m2) | 0.6 | 0.5 | 0.24 | 0.15 | 0.05 | 0.025 | 0.02 | 0.007 |
Km factor | 20 | 20 | 12 | 12 | 8 | 6 | 5 | 3 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × | mouse Km(3) | = 11.2 mg/kg |
rat Km(6) |
Chemical Information
Molecular Weight (MW) | 309.33 |
---|---|
Formula | C15H15N7O |
CAS No. | 1224844-38-5 |
Storage | 3 years -20℃Powder |
---|---|
6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | |
Solubility (25°C) * | In vitro | DMSO | 62 mg/mL (200.43 mM) |
---|---|---|---|
Water | <1 mg/mL ( | ||
Ethanol | 2 mg/mL (6.46 mM) | ||
In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol | 30 mg/mL | |
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Chemical Name | 3-(2-aminobenzo[d]oxazol-5-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine |
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Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on INK 128 1224844-38-5. We are ready to answer your questions on packaging, logistics, certification or any other aspects about MLN0128 1224844-38-5、1224844-38-5 INK 128. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : PI3K/Akt/mTOR > mTOR Inhibitor
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