TAK-733 1035555-63-5
Product Description
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Molecular Weight:
504.23 TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1.
Biological Activity
TAK-733 is highly potent and selective MEK allosteric site inhibitor
with IC50 of 3.2 nM. TAK-733 shows potent enzymatic and cell activity
with an EC50 of 1.9 nM against ERK phosphorylation in cells.
TAK-733 demonstrates broad antitumor activity in mouse xenograft models
of human cancer including models of melanoma, colorectal, NSCLC,
pancreatic and breast cancer. TAK-733 is well tolerated with
pharmacokinetics and pharmacodynamics that support once-daily oral
dosing in humans. TAK-733 shows maximally efficacious doses at once
daily orally doses of 10 mg/kg.
Protocol(Only for Reference)
Animal Study: [2]
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
Molarity Calculator
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Contact us if you need more details on 1035555-63-5. We are ready to answer your questions on packaging, logistics, certification or any other aspects about TAK-733 1035555-63-5、1035555-63-5 TAK-733. If these products fail to match your need, please contact us and we would like to provide relevant information.
Molecular Weight:
504.23 TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1.
Biological Activity
TAK-733 is highly potent and selective MEK allosteric site inhibitor
with IC50 of 3.2 nM. TAK-733 shows potent enzymatic and cell activity
with an EC50 of 1.9 nM against ERK phosphorylation in cells.
TAK-733 demonstrates broad antitumor activity in mouse xenograft models
of human cancer including models of melanoma, colorectal, NSCLC,
pancreatic and breast cancer. TAK-733 is well tolerated with
pharmacokinetics and pharmacodynamics that support once-daily oral
dosing in humans. TAK-733 shows maximally efficacious doses at once
daily orally doses of 10 mg/kg.
Protocol(Only for Reference)
Animal Study: [2]
Animal Models | Human solid tumor xenograft models including NSCLC (NCI H23 [KRAS and LKB1 mutations]), CRC (SW620 [KRAS, APC, p53 mutations]) Pancreatic cancer (Panc 1 and Capan 1 [KRAS mutations] and BxPC-3 [No MAPK mutations]) models in immunocompromised mice. |
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Formulation | Saline |
Dosages | 10 mg/kg |
Administration | Orally administrated once daily for 21 days |
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) | 504.23 |
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Formula | C17H15F2IN4O4 |
CAS No. | 1035555-63-5 |
Storage | 3 years -20℃Powder |
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6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | |
Solubility (25°C) * | In vitro | DMSO | 101 mg/mL (200.3 mM) |
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Water | <1 mg/mL ( | ||
Ethanol | <1 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 | (R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione |
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Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on 1035555-63-5. We are ready to answer your questions on packaging, logistics, certification or any other aspects about TAK-733 1035555-63-5、1035555-63-5 TAK-733. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : MAPK > MEK Inhibitor
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